Inhibitor Suppliers USA
Find where to buy products from suppliers in the USA, including: distributors, industrial manufacturers in America, bulk supplies and wholesalers of raw ingredients & finished goods.
Search for products or services, then visit the American suppliers website for prices, SDS or more information. You can also view suppliers in Australia, NZ or the UK.
Product | Description | |
---|---|---|
Inhibitor Library Quick inquiry Where to buy Suppliers range | A unique collection of 5700 inhibitors for research in cell signaling, high throughput screening (HTS) and high content screening (HCS) for new drugs; - Bioactivity and safety confirmed by pre-clinical research and clinical trials, and some of them are approved by FDA; - Covers various major targets including MAPK, PI3K, JAK, HDAC, VEGFR, CDK, etc. ; - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2000. Categories: Inhibitor Libraries. | |
BMP Inhibitor III, LDN-212854 (Abl Inhibitor V, LDN212854, Bone Morphogenetic Protein Inhibitor III, PDGFR Tyrosine Kinase Inhibitor XXIV, RIP2 Inhibitor I, RIPK2 Inhibitor I, 5-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrazolopyrimidinyl quinoline that is superior to Dorsomorphin and DMH1 as an ATP-site-targeting, ALK1/2 inhibitor (IC50 = 2.40 and 1.30nM, respectively; [ATP] = 6uM) with respect to both potency and selectivity over ALK3/4/5 (IC50 = 0.858, 2.133, and 9.276uM, respectively). Also a potent RIPK2 inhibitor (IC50 = 6nM) with reduced potency against ABL1/c-abl, PDGFR-beta, ALK3, and PDGFR-alpha (IC50 = 40, 68, 85.8, and 650nM, respectively) and little inhibitory activity toward a panel of more than 190 kinases. Effectively inhibits ALK2- and ALK3-mediated C2C12 osteogenic differentiation (IC50 = 10 and 40.5nM, respectively) in vitro and prevents constitutively active ALK2 Q207D mutant-induced heterotopic ossification in mice (6mg/kg/12h via i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H??N?. US Biological Life Sciences. | Worldwide |
Histone Acetyltransferase Inhibitor VIII, NU9056 (1,2-Bis(isothiazol-5-yl)disulfane, 1,2-di(isothiazol-5-yl)disulfane, KAT5 Inhibitor I, Tip60 Inhibitor I, HAT Inhibitor VIII, p300/CBP Inhibitor VII, PCAF Inhibitor V) Quick inquiry Where to buy Suppliers range | A cell-permeable disulfane compound that is reported to be more potent against KAT5/Tip60 than PCAF, p300, and GCN5 in cell-free HAT activity assays (IC50 ≤2, ≤36, ≤60, and >100uM, respectively) and effectively reduce H3K14, H4K8, H4K16, but not alpha-tubulin, acetylation level in LNCaP prostate cancer cells (max inhibition at 5-10uM). Shown to induce cell cycle arrest and apoptosis (17 to 24uM) in LNCaP cultures and exhibit antiproliferation activity in both androgen-responsive and androgen-independent CaP cultures (GI50 from 7.5 to 27uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C?H?N?S?, Primary Target: KAT5. US Biological Life Sciences. | Worldwide |
ATIC Dimerization Inhibitor (Ac-Arg-Ph(4-NO2)-NEt2, ATIC Inhibitor, AICAR Tfase Inhibitor, AICAR Transformylase Inhibitor, AICAR Tranformylase/Inosine Monophosphate Cyclohydrolase Dimerization Inhibitor, AMPK Signaling Activator XI) Quick inquiry Where to buy Suppliers range | A cell-permeable dipeptide that reversibly blocks the homodimerization of aminoimidazole carboxamide ribonucleotide transformylase/inosine nomophosphate cyclohydrolase (ATIC) and inhibits its activity (Ki = 691nM, Kd = 240nM). AITC is a bifunctional enzyme that catalyzes the last two steps of de novo purine biosynthesis. Increases the intracellular levels of AICAR leading to the activation of AMP-activated protein kinase (AMPK). Shown to reduce cell viability in a dose-dependent manner. Exhibits a longer half-life and sustained AMPK activation (~24h), compared to AICA-riboside. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences. | Worldwide |
Cancer Hydrolase KIAA1363 Inhibitor, JW480 (2-Isopropylphenyl-2- (2-naphthyl) ethylcarbamate, AADACL1 Inhibitor, Arylacetamide Deacetylase-Like 1 Inhibitor, NCEH1 Inhibitor, Neutral Cholesterol Ester Hydrolase 1 Inhibitor) Quick inquiry Where to buy Suppliers range | A membrane-permeable, highly potent and selective inhibitor against the 2-acetyl MAGE (monoakylglycerol ether) hydrolase KIAA1363/AADACL1 of both human (IC50=12nM; PC3 lysate) and murine (IC50=20nM; brain membrane samples) origin, with no significant effect toward other PC3 or murine brain serine hydrolase activities, including HSL, FAAH, and AChE. Readily crosses blood-brain barrier in mice and effectively suppresses PC3-derived tumor growth in mice in vivo (by 56% on day 33; 80mg/kg/day; o.g.). Also inhibits blood carboxylesterase. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
CRM1 Inhibitor IV, KPT-251 (KPT251, (Z) -2- (2- (3- (3, 5-bis (trifluoromethyl) phenyl) -1H-1, 2, 4-triazol-1-yl) vinyl) -1, 3, 4-oxadiazole, Exportin 1 Inhibitor IV, Chromosome Region Maintenance 1 Protein Inhibitor IV, CRM1 Inhibitor IV, XPO1 Inhibitor IV) Quick inquiry Where to buy Suppliers range | A cell-permeable, irreversible, triazole-containing heterotricyclic CRM1 inhibitor that effectively blocks CRM1-mediated nuclear export (4h 1uM in U2OS cells) via covalent interaction with CRM1 NES- (nuclear export signal) binding groove cysteine (Cys528 in human). Exhibits antileukemic activity against primary human CD19+ CLL (IC50 <500nM) via apoptosis induction even in the presence of stroma cells or other known CLL survival stimuli, while exhibiting little cytotoxicity toward CD56+ NK cells from healthy donors (1uM; up to 72h). Reported to prolong the survival of SCID mice (75mg/kg p.o.) engrafted with murine E-mu-TCL1 or human MV4-11 leukemia in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H?F?N?O. US Biological Life Sciences. | Worldwide |
Glutaminase Inhibitor, Compound 968 (5- (3-Bromo-4- (dimethylamino) phenyl) -2, 2-dimethyl-2, 3, 5, 6-tetrahydrobenzo [a]phenanthridin-4 (1H) -one, GAC Inhibitor, GLS1 Inhibitor I, KGA Inhibitor I, Kidney-Type Glutaminase Inhibitor I) Quick inquiry Where to buy Suppliers range | A cell-permeable benzophenanthridinone compound that acts as an allosteric and reversible inhibitor of mitochondrial glutaminase activity and represses the growth and invasive activity in glutaminase upregulated fibroblasts and in tumor cells (IC50 <10uM in NIH3T3 cells stably expressing Dbl, Cdc42-F28L, Rac-F28L or RhoC-F30L mutants and in SKBR3 and MDA-MB231 cancer cells). Shown to effectively shrink tumor size in P-493 B xenografted mouse model (200 µg per inj. i.p., 12 days). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Heat Shock Factor 1 Inhibitor, KRIBB11 (N2-(1H-Indazol-5-yl)-N6-methyl-3-nitropyridine-2,6-diamine , HSF1 Inhibitor, KRIBB11, Heat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor, Hsp70 Induction Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell-permeable 2,6-diaminopyridine compound that directly binds HSF1 and reversibly inhibits its transcriptional activity (IC50=1.2uM in heat shocked p[HSE]4-Ta-Luc transfected HCT-116 cells), and suppresses both the transcription and expression of hsp70, hsp47 and hsp27. Shown to block heat shock-induced p-TEFb (positive transcription elongation factor b) recruitment to the hsp70 promoter and inhibit the phosphorylation of RNA Pol II CTD-Ser2 with no effect on TNF-a-stimulated NF-kB activity in HeLa cells. Induces G2/M growth arrest and apoptosis (IC50 ~5uM in HCT-116 cells), and further decreases tumor growth in mouse xenograft regression model (50mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
JQ1 Enantiomers Set ((S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate, SGCBD01, BRD2 Inhibitor III, BRD3 Inhibitor II, BRD4 Inhibitor III, BRD6 Inhibitor I, BRDT Inhibitor I) Quick inquiry Where to buy Suppliers range | A cell-permeable I-BET class of thienodiazepine derivative whose (S)-(+), but not (R)-(-), enantiomer is shown to target both bromodomains (BD1 & BD2) of BET family members BRD2, BRD3, BRD4, and BRD6/BRDT in a Kac- (epsilon-N-acetylated lysine) competitive manner, exhibiting little affinity toward 23 other BD-containing proteins, BRD1 and BRD9, and little or no activity against a panel of more than 50 receptors, ion channels, and transporters. Effectively inhibits the oncogenic BRD4-NUT fusion-dependent NUT midline carcinoma and c-Myc oncoprotein-dependent multiple myeloma proliferation both in cultures (IC50 <1uM) in vitro and in mice (50mg/kg/day i.p.) in vivo. Also reported to cross the blood-testis boundary in male mice and effectively block BRDT-mediated spermatogenesis without affecting hormone levels. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1set. US Biological Life Sciences. | Worldwide |
Lactate Dehydrogenase A Inhibitor, FX11 (LDHA Inhibitor I, LDH-A Inhibitor I, LDH-M Inhibitor I, LDHM Inhibitor I) Quick inquiry Where to buy Suppliers range | A cell permeable, gossypol analog that acts as a selective, reversible, and NADH competitive inhibitor of lactate dehhydrogenase A (LDHA; Ki = 8uM for human liver LDHA). Does not affect the activities of LDHB and glyceraldehyde-3-phosphate dehydrogenase even at higher concentrations. Shown to increase oxygen consumption, reactive oxygen species production, and cell death in P493 human lymphoma B cells. Also shown to reduce mitochondrial transmembrane potential and ATP levels and increase AMP kinase activity. Exhibits synergistic toxicity in P493 cells when combined with FK866. Blocks the progression of human lymphoma and pancreatic cancer xenografts and when used in combination with FK866 it induces lymphoma regression. Group: Biochemicals. Grades: Highly Purified. CAS No. 213971-34-7. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
LRRK2 Inhibitor III, HG-10-102-01 (Leucine-Rich Repeat Kinase 2 Inhibitor III, Mixed-Lineage Kinase 1 Inhibitor I, MLK1 Inhibitor I, MNK Inhibitor III, (4- (5-Chloro-4- (methylamino)pyrimidin-2-ylamino)-3-methoxyphenyl) (morpholino)methanone) Quick inquiry Where to buy Suppliers range | A cell-permeable 2,4-diaminopyrimidinyl compound that acts as a potent, ATP-competitive LRRK2-selective inhibitor (IC5050 = 20.3, 3.2, 153.7 and 95.9nM, respectively,against human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant; [ATP] = 100uM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1uM, respectively; [ATP] = 100uM) and little activity toward a panel of 136 other kinases. Although both HG-10-102-01 and LRRK2-In-1 inhibit cellular wt and G20195 LRRK2 phosphorylation (Optimal conc. 1 to 3uM), only HG-10-102-01 is effective against cellular A2016T and G2019S/A2016T LRRK2 phosphorylations (IC50 <3uM). And only HG-10-102-01, but not LRRK2-In-1 or CZC-25146, can cross blood-brain-barrier for LRRK2 phosphorylation inhibition in mice (30mg/kg to 50mg/kg i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?O?. US Biological Life Sciences. | Worldwide |
LSD1 Inhibitor IV, RN-1,HCl (2- (1R, 2S) -2- (4- (Benzyloxy) phenyl) cyclopropylamino) -1- (4-methylpiperazin-1-yl) ethanone, HCl, Lysine (K)-Specific Demethylase Inhibitor IV,RN-1,HCl, BHC110 Inhibitor IV, KDM1 Inhibitor IV, MOA Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable tranylcypromine (parnate) analog that acts as a potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC50=70nM in a HRP-coupled assay using H3K4Me2 peptide substrate). Forms a covalent adduct with flavin adenine dinucleotide (FAD). Shown to cross the blood brain barrier. Exhibits moderate selectivity over amine oxidases MAO-A and MAO-B (IC50=0.51 and 2.785uM, respectively). Displays desirable pharmacokinetic properties (brain/plasma exposure ratio of 88.9), and impairs long-term memory without affecting short-term memory in mice (10mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Akt Inhibitor XVI, AT7867 (p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, Chlorophenyl-pyrazolyl-phenyl-piperidine, S6K1 Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20nM), and p70S6K (IC50 = 85nM) in an ATP-competitive manner (Ki = 18nM using AKT2), with much reduced potency toward RSK1 (IC50 >100nM) and a panel of 13 other cellular kinases (IC50 >1uM). Shown to reduce cellular phosphorylation of GSK-3beta (IC50 range from 2.08 to 4.45uM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86uM) and in mice in vivo (20mg/kg via i.p. or 90mg/kg via p.o.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?. US Biological Life Sciences. | Worldwide |
Casein Kinase II Inhibitor VIII (4- (2- (4-Methoxybenzamido) thiazol-5-yl) benzoic acid, CK2 Inhibitor VIII, DYRK1B Inhibitor, Flt-3 Inhibitor VII) Quick inquiry Where to buy Suppliers range | A cell-permeable thiazolamide compound that acts as a potent, reversible, and ATP-competitive inhibitor against casein kinase-2/CK2 (IC50=32 and 46nM against CK2a and CK2a', respectively), as well as DYRK1B and FLt-3 (82% and 76% inhibition, respectively, at 30nM), while diplaying reduced or little potency toward other targets in a 70-kinase panel selectivity profile study. Shown to effectively block the proliferation of a variety of cancer cells (IC50=2.6, 1.6, and 2.4uM, in A549, HCT116, and MCF-7 cultures, respectively). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
CRM1 Inhibitor III (Chromosome Region Maintenance 1 Protein Inhibitor III, (Z)-But-2-enedioic acid (4-bromophenyl)amide (3-chlorophenyl)amide, Exportin 1 Inhibitor III, XPO1 Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable butenediamide compound that acts as a potent, active site cysteine reactive irreversible inhibitor of CRM1/exportin 1. Shown to selectively repress agonist-mediated nuclear export of HDAC4/5, Rev and NFAT proteins in neonatal rat ventricular myocytes (NRVMs; EC50=2.2 and 3.5nM for GFP-HDAC5 and GFP-HIV Rev) and suppress hypertrophic growth of NRVMs (EC50=52nM for ANF expression inhibition) with negligible effect either on the phosphorylation of HDAC5 or on the kinase activities of P and CaMKII at 1uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??BrClN?O?. US Biological Life Sciences. | Worldwide |
EBP1 Inhibitor, WS6 (N- (6- (4- (2- (4- ( (4- methyl piperazin-1-yl) methyl ) -3- (trifluoro methyl ) phenylamino) -2-oxoethyl) phenoxy) pyrimidin-4-yl) cyclopropane carboxamide, xHCl, Erb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable phenoxypyrimidin-cyclopropane carboxamide compound that effectively stimulates the growth of primary beta cells in cultured primary rat and human islets in vitro (ECmax in 4 d = 200 and 400nM, respectively) and in the murine type 1 diabetes (T1D) model RIP-DTA in vivo (170% of control pancreas Ki-67-positive beta cells in 1 wk; 5mg/kg i.p. q.o.d.) by interacting with IKKε and EBP1/PA2G4/Erb3 binding protein-1 and blocking the known suppressor function of EBP1 toward E2F-mediated transcription. Likewise, dual inhibition of EBP1 (with shRNA) and IKK (1uM) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O?; xHCl. US Biological Life Sciences. | Worldwide |
JAK Inhibitor I (P6, DBI, (2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, JAK1 Inhibitor I, JAK3 Inhibitor VII, JAK2 Inhibitor I) Quick inquiry Where to buy Suppliers range | A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50=15nM for murine JAK1), JAK2 (IC50=1nM), JAK3 (Ki=5nM), and Tyk2 (IC50=1nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490. A 10mM solution of JAK Inhibitor I in DMSO is also available. Group: Biochemicals. Grades: Highly Purified. CAS No. 457081-03-7. Pack Sizes: 500ug, 1mg. US Biological Life Sciences. | Worldwide |
MARK/Par-1 Activity Inhibitor, 39621 (N-(2,5-Dimethylphenyl)-2-(4-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrazin-2-ylthio)acetamide, Microtubule Affinity Regulating Kinase Inhibitor, MAP Affinity Regulating Kinase Inhibitor, PAR1 Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK-selective inhibitor (IC50=3.6uM; [ATP]=100uM). Shown to effectively block primary rat cortical neuron axon growth (5.7um/hr vs 32.5um/hr with or without 20uM inhibitor) and prevent MARK2 overexpression-induced Tau Ser262 phosphorylation and cytotoxicity in CHO cells (10uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Mer RTK Inhibitor, UNC569 (1- ( (trans-4-Aminocyclohexyl) methyl) -N-butyl-3- (4-fluorophenyl) -1H-pyrazolo[3, 4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I) Quick inquiry Where to buy Suppliers range | An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50=2.9nM; Ki=4.3nM) with ~10-fold greater selectivity over other TAM family kinases (IC50=37 and 48nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC50 of 141nM. Exhibits desirable pharmacokinetic profile and efficacy in mice. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
mTOR Inhibitor XII, Torin2 (9- (6-aminopyridin-3-yl) -1- (3- (trifluoromethyl) phenyl) benzo[h][1, 6]naphthyridin-2 (1H) -one, DNA-PK Inhibitor VII, PI 3-K Inhibitor XIX, PI 4-K Inhibitor) Quick inquiry Where to buy Suppliers range | A Torin1 structural analog that acts as a cell-permeable, potent, ATP-competitive inhibitor against DNA-PK and mTOR (IC50 = 0.5 and 2.81nM, respectively). Comparing to Torin1, Torin2 displays enhanced inhibitory potency against PI 4-Kbeta (IC50 = 18.3nM) and PI 3-K (IC50 =4.68, 5.67, 8.58, 17.5, 24.5, and 28.1nM, respectively, against P110alpha/P85alpha, P110-gamma, hVPS34, P110delta/P85alpha, C2beta, C2alpha, respectively), while being more effective in inhibiting S6K1 Thr389 phosphorylation in MEF cultures (IC50 = 0.25nM vs 2nM, respectively, for Torin2 and Torin1) in vitro and displaying much improved oral bioavailability in mice (Cmax (ng/mL) /T1/2 (h) = 3968/0.72 and 223/0.79, respectively, for Torin2 and Torin1; 10/mg/kg p.o.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??F?N?O, Primary Target: MTOR. US Biological Life Sciences. | Worldwide |
NF-kB Activation Inhibitor VIII, EVP4593 (SOC Inhibitor, Neuronal Store-Operated Calcium Entry Inhibitor, N4- (4-phenoxyphenethyl) quinazoline-4, 6-diamine, TRPC1 Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-kB activation in Jurkat cells (IC50=11nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30nM to 3uM, which is consistent with TRPC1 knocown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100uM to 400uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
p300/CBP Inhibitor VI, L002 (4- (4-Methoxyphenyl sulfonyl oxyimino) -2, 6-di methyl -2, 5-cyclohexadien-1-one, GCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV) Quick inquiry Where to buy Suppliers range | A cell-permeable phenyl sulfonyl oxyimi nocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98uM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500ug/100ul, i.p. twice a week). Group: Biochemicals. Grades: Highly Purified. CAS No. 321695-57-2. Pack Sizes: 10mg. Molecular Formula: C??H??NO?S. US Biological Life Sciences. | Worldwide |
PKR Inhibitor III, 7DG (Double-stranded RNA-activated Protein Kinase Inhibitor III, EIF2AK2 Inhibitor III, 7-Desacetoxy-6,7-dehydrogedunin, Double-stranded RNA-dependent Protein Kinase Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable gedunin analog that directly targets PKR via reversible interaction inhibits PKR-mediated cellular events by disrupting PKR signaling complexes assembly, such as IkK complex and inflammasome / pyroptosome, resulting in effective blockage of LPS-induced IkBbeta degradaion (20uM) and protection against anthrax toxin LT-induced caspase-1 activation as well as subsequent pyroptosis (10uM) in murine macrophage J774 cultures. PKR is also known to mediate LT-induced apoptosis via its kinase activity in LPS-primed Macrophages derived from C57BL/6 with a resistent NLRP1 allele, inhibitable by C16, but not by 7DG, while LT-induced pyroptosis in J774 cultures is insensitive to C16 treatment. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H??O?. US Biological Life Sciences. | Worldwide |
SRPK Inhibitor, SRPIN340 (N- (2-Piperidin-1-yl-5- (trifluoromethyl) phenyl) isonicotinamide, Serine-Arginine-Rich Protein Kinase Inhibitor, SR Protein Kinase Inhibitor, SR Protein Phosphorylation Inhibitor 340, (SRPIN)340) Quick inquiry Where to buy Suppliers range | A cell-permeable isonicotinamide that acts as an ATP-competitive SRPK1-selective inhibitor (IC50 = 0.14 and 1.8uM, respectively, against mSRPK1 and mSRPK2) with much reduced activity against 143 other kinases. Shown to effectively counteract IGF-1-induced anti-angiogenic to pro-angiogenic VEGF isoforms switch both in cultures in vitro (1h 10uM SRPIN340 prior to 12h IGF-1 stimulation of PCIPs) and in a murine hypoxia-induced retinal neovascularization model in vivo (10pmol/uL/eye intraocular SRPIN340 injection) by inhibiting PKC/SRPK signaling-dependent, alternate splicing factor ASF- (SF2; splicing factor 2) mediated VEGF pro-mRNA PSS (proximal splice site) selection. Suppresses RNA virus Sindbis propagation (IC50 = 60uM in Vero cultures) and HCV-JFH1 replication (1 & 10uM SRPIN340 in Huh7.5.1 cultures). Exhibits no toxicity toward rats (2g/kg p.o. for 2 wks), CHO (5mg/ml for 24h), or Huh7 (30uM for 48h). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
APE1 Inhibitor III (Apurinic Endonuclease 1 Inhibitor III) (Apurinic/Apyrimidinic Endonuclease 1 Inhibitor III)(N-(3-(1,3-Benzo[d]thiazol-2-yl)-6-isopropyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl)acetamide) Quick inquiry Where to buy Suppliers range | A cell-permeable benzothiazolyltetra hydrothienopyridine compound that acts as a potent, competitive, and active site targeting inhibitor of APE1 (IC50=2.0uM in a fluorescence based HTS assay; and 12uM in a radiotracer incision assay). Shown to block APE1 activity in HEK293T and HeLa cells extract (IC50=600nM) and increase genomic AP site accumulation. Potentiates the cytotoxicity of DNA-damaging alkylating agents in HeLa cells by ~3-fold. Exhibits favorable pharmacokinetic properties and desirable ADME attributes. Due to its lipophilic nature, it crosses the blood-brain barrier rather easily and shows desirable stability (t1/2=80min). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
ATR/CDK Inhibitor, NU6027 (2,6-diamino-4-cyclohexyl-methyloxy-5-nitroso-pyrimidine, ATR Inhibitor, NU6027, CDK2 Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable, pyrimidine derivative that acts as an ATP-competitive CDK Inhibitor (Ki=2.5uM for CDK1, and Ki=1.3uM for CDK2), and demonstrates cytostatic properties among a panel of 57 cancer cell lines. Also inhibits ATR kinase (IC50=6.7uM in MCF7 cells), but does not interfere with irradiation-induced autophosphorylation of DNA-PK or ATM. Potentiates a range of DNA-damaging cytotoxic drugs such as hydroxyurea (1.8-fold) and cisplatin (1.4-fold) at 10uM, but not the anti-mitotic paclitaxel. Attenuates G2/M arrest following DNA damage and inhibits RAD51 focus formation. Shown to be synthetically lethal when DNA single-strand break repair is impaired in PARP-inhibited cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 220036-08-8. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
BMP Inhibitor II, DMH1 (ALK2/3 Inhibitor, DMH1, Bone Morphogenetic Protein Inhibitor, DMH1, 4- (6- (4-Isopropoxyphenyl) pyrazolo[1, 5-a]pyrimidin-3-yl) quinoline) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrrazolopyrimidine compound that inhibits against R/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50=25.1, 148, and 234.6nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFbR-I, ZAPK, Syk, PKCth, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100=2.5uM) and VEGF signaling-dependent intersomitic vessel formation (EC50=5uM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR and/or Metformin for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 1206711-16-1. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
CARM1 Inhibitor (1-Benzyl-3, 5-bis- (3-bromo-4-hydroxybenzylidene) piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, PRMT Inhibitor V) Quick inquiry Where to buy Suppliers range | A cell-permeable (bis-benzylidene) piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50=7.1uM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100uM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50>100uM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100uM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6uM inhibitor). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Casein Kinase II Inhibitor XII, TBBz (4, 5, 6, 7-Tetra bromobenzimidazole, CYP24A1 inhibitor, TBBz, CK2 Inhibitor, TBBz) Quick inquiry Where to buy Suppliers range | A cell-permeable halogenated benzimidazole compound that acts as a selective and ATP competitive inhibitor of casein kinase II (CK2, Ki = 70nM for the active hetero-tetrameric form). However, its effect on free CK2a and CK2a' subunits is significantly reduced (Ki = 510 and 400nM, respectively). Reported to reduce viability and proliferation in HeLa, Jurkat, and HL-60 cells (at 25uM). Also shown to disrupt the promoter activity of CYP24A1 and down-regulates its endogenous and 1, 25-Vitamin D3 (1,25-D3)-induced expression in PC3 cells. Synergistically enhances the anti-tumor effect of 1, 25-D3 in a PC3 xenograft murine model. CAS No:577779-57-8. Group: Biochemicals. Grades: Highly Purified. CAS No. 577779-57-8. Pack Sizes: 20mg. Molecular Formula: C?H?Br?N?, Primary Target: CK2. US Biological Life Sciences. | Worldwide |
DUB Inhibitor IV, b-AP15 (NSC687852, 3, 5-bis ( (4-Nitrophenyl) methylidene) -1-prop-2-enoylpiperidin-4-one, (3E, 5E) -1-Acryloyl-3, 5-bis (4-nitrobenzylidene) piperidin-4-one, USP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell-permeable bis-nitrobenzylidene-piperidinone compound that acts as a potent, reversible and selective inhibitor of 19S regulatory-particle-associated deubiquitylating enzymes (DUBs) UCH-L5 and USP-14 (IC50=2.1uM against Ub-AMC substrate), with no effect on UCH-L1, UCH-L3, USP2, USP7, USP8 and BAP1 and on the proteasomal proteolytic activities. Shown to prevent proteasomal degradation (IC50=0.8uM in MelJuSo-UbG76V-YFP cells), and cause accumulation of higher molecular weights polyubiquitinated proteins in HCT-116 cells. Preferentially induces cell-cycle arrest and apoptosis in several colon cancer and in CNS cells, and effectively suppresses tumor growth in various mouse model (5mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. CAS No. 1009817-63-4. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?, Molecular Weight: 419.4. US Biological Life Sciences. | Worldwide |
DUB Inhibitor VI, P22077 (1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone, USP7 Inhibitor II, USP47 Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50=8.01 & 8.74uM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 targets (IC50 >50uM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150uM; 0.5 to 20h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences. | Worldwide |
eIF2-GTP-tRNAiMet Ternary Complex Inhibitor, BTdCPU (N,N'-diarylurea;translation Initiation Tenrary Complex Inhibitor, 1-(benzo[d][1, 2, 3]thiadiazol-6-yl)-3-(3, 4-dichlorophenyl)urea, BTdCPU, Heme-regulated Inhibitor Kinase Activator, BTdCPU) Quick inquiry Where to buy Suppliers range | A cell-permeable N,N'-diarylurea that acts as an inhibitor of the formation of the ternary complex of eukaryotic translation initiation factor 2 (eIF2), GTP and the initiator methionine tRNA (Met-tRNAi), a key regulatory step of translation initiation. It directly activates heme-regulated inhibitor kinase (HRI), which then phosphorylates eIF2a in cells at 10uM and in cell-free extracts dose-dependently, and thereby prevents respective ternary complex formation without elevating oxidative stress. The sensitivities of various cancer cell lines to the anti-proliferative effects of this compound are shown to correlate with the expression of HRI. Furthermore, this compound displays tumor growth inhibition in a mice xenograft model of MCF-7 human breast cancer cells at 175mg/kg, in vivo.CAS No:1257423-87-2. Group: Biochemicals. Grades: Highly Purified. CAS No. 1257423-87-2. Pack Sizes: 10mg. Molecular Formula: C??H?Cl?N?OS, Molecular Weight: 339.2. US Biological Life Sciences. | Worldwide |
Ezh2 Inhibitor II, EI1(Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI, 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide) Quick inquiry Where to buy Suppliers range | A cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2 / SUZ12 / EED / AEBP2 / RbAP48) HMTase activity (IC50/substrate = 15nM/H3K27me021-44 and 13nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1uM) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50 = 1.34uM) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50 >100uM). Shown to suppress cellular H3K27 dimethylation and trimethylation (1 to 10uM) in DLBCL cultures and exhibit antiproliferation activity against DLBCL cell lines with wt or mutant Ezh2 (3.3uM to 10uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?, Primary Target: Ezh2/PRC2. US Biological Life Sciences. | Worldwide |
Fbxo3 Inhibitor, BC-1215 (N1,N2-bis(4-(Pyridin-2-yl)benzyl)ethane-1,2-diamine, F Box Only Protein 3 Inhibitor, F Box Protein 3 Inhibitor, BC1215, F Box and Leucine-rich Repeat Protein 2 Activator, Fbxl2 Activator) Quick inquiry Where to buy Suppliers range | A cell-permeable, bis-pyridinyl benzyl ethanamine that disrupts Fbxo3-Fbxl2 interaction and effectively prevents SCF-Fbxo3-catalyzed Fbxl2 ubiquitination, resulting in cellular Fbxl2 upregulation and thereby SCF-Fbxl2-catalyzed TRAFs (TNF Receptor-Associated Factors) ubiquitination. Effectively reduces cellular TRAFs (5 to 127uM) and prevents TRAF-mediated cytokines production from LPS-stimulated human PBMC (25uM). Shown to greatly prevent Cecal Ligation & Puncture-induced plasma cytokine elevation and substantially reduce the severity of lung inflammation post intratracheal P. aeruginosa infection in mice (100ug/mouse; i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?, Primary Target: Fbox3. US Biological Life Sciences. | Worldwide |
Hdm2 E3 Ligase Inhibitor II, HLI373 (5- (3-Dimethylaminopropyl amino) -3, 10-dimethyl-10H-pyrimido [4, 5-b] quinoline-2, 4-dione, 2HCl, MDM2 Inhibitor VI, MDM2 E3 Ligase Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrimidoquinoline-dione compound that acts as an efficient Hdm2 E3 ligase inhibitor, prevents Hdm2-mediated p53 ubiquitination and increases the cellular levels of both p53 and Hdm2 (IC50 ~3uM in RPE cells). Shown to selectively arrest the growth of several tumor cells in a p53-dependent manner and display desirable aqueous solubility. Group: Biochemicals. Grades: Highly Purified. CAS No. 502137-98-6. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
IRE1 Inhibitor III, 4u8C (8-Formyl-7-hydroxy-4-methylcoumarin, 7-Hydroxy-4-methyl-2-oxo-2H-chromene-8-carbaldehyde, ER-to-Nucleus Signaling 1 Inhibitor III, Inositol-Reguiring Protein 1 Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable coumarin o-hydroxyaldehyde that inhibits IRE1 RNase activity in a time- and dose-dependent manner (IC50=550 and 45nM, respectively, with 0 and 16min drug preincubation in RNA cleavage assays) by covalently targeting IRE1 Lys907 via Schiff base formation, effectively preventing ER stress-induced site-specific mRNA splicing as well as RIDD (Regulated IRE1-Dependent Degradation) mRNA degradation (IC50=6.9 and 4.1uM, respectively, against Xbp1 splicing and Scara3 degradation) in MEF cultures following Tunicamycin treatment. Comparing to STF083010, 4u8C is also shown to inhibit IRE1 autophosphorylation in cell-free assays via Schiff base formation with IRE1 Lys599 in the absence of ADP, however cellular nucleotide prevents 4u8C from targeting IRE1 Lys599 intracellularly. Group: Biochemicals. Grades: Highly Purified. CAS No. 14003-96-4. Pack Sizes: 25mg. US Biological Life Sciences. | Worldwide |
KMO Inhibitor I, Ro 61-8048 (Kynurenine-3-Monooxygenase Inhibitor I, Ro 61-8048 3,4-Dimethoxy-N-[4-(3-nitrophenyl)-2-thiazolyl]-benzenesulfonamide Dimethoxy-nitrophenyl-thiazolyl-benzenesulfonamide, Kynurenine-3-Hydroxylase Inhibitor I, Ro 61-8048) Quick inquiry Where to buy Suppliers range | A cell-permeable thiazolyl Benzene sulfonamide compound that acts as a potent, competitive and reversible inhibitor of kynurenine-3-monooxygenase activity (Ki=4.8nM; IC50=37nM). Reported to increase the circulating levels of kynurenic acid (KYNA), an excitatory amino acid receptors antagonist, lower reactive oxygen species [ROS], reduce neuronal loss and enhance the survival rate in several neuronal disease models. An orally bioavilable KMO Inhibitor II, JM6, a prodrug of Ro 61-8048 is also available. Group: Biochemicals. Grades: Highly Purified. CAS No. 199666-03-0. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S?, Molecular Weight: 421.5. US Biological Life Sciences. | Worldwide |
MDM2/MDMX Dual Inhibitor, RO-5963 ((Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide, MDM2 Inhibitor VII, MDMX Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable indolyl-hydantoin compound that simultaneously inhibits the interaction of both, MDM2 and MDMX with p53 (IC50 = 17.3 and 24.7nM, respectively, in vitro). Releases p53 from MDMX inhibition, stabilizes it, and fully restores its function. Shown to be far more superior to Nutlin-3a in blocking p53 interaction with MDMX. Binds to Phe, Trp, and Leu sub-pockets on the surface of MDMX and MDM2, and promotes MDMX and MDM2 dimer formation. Shown to induce cell cycle arrest in G1 and G2 phases. Also reported to induce apoptosis in several tumor cell lines expressing wild-type p53/MDMX (~10-20uM). Its actions are not believed to be due to any genotoxic stress. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
MLKL Inhibitor, Necrosulfonamide ((E)-N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide, Mixed Lineage Kinase Domain-like Protein Inhibitor, Necrosome Inhibitor II, Necrosulfonamide) Quick inquiry Where to buy Suppliers range | A cell-permeable acrylamide compound that inhibits human, but not murine, MLKL adaptor function via covalent modification of Cys86 and is more potent than Nec-1 in preventing necrotic/necroptotic death in human HT-29 (IC50 = 124nM and 2uM, respectively), being ineffective against necrosis/necroptosis in murine L929 or apoptosis in human RIP3-null Panc-1 cells. Unlike Nec-1, which prevents necrosome formation by blocking RIP1-RIP3 interaction, MLKL prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with further downstream effectors. Group: Biochemicals. Grades: Highly Purified. CAS No. 432531-71-0. Pack Sizes: 25mg. Molecular Formula: C??H??N?O?S?, Primary Target: human MLKL. US Biological Life Sciences. | Worldwide |
MNK1/2 Inhibitor II, ETP-45835 (ETP45835?MNK Inhibitor II, Mitogen-Activated Protein Kinase-Interacting Kinase Inhibitor II) (4-(3-(Piperidin-4-yl)-1H-pyrazol-5-yl)pyridine, diHCl) Quick inquiry Where to buy Suppliers range | A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC50=646 and 575nM, respectively, against MNK1 and MNK2) with much reduced or little activity against 24 other kinases (<15% inhibition at 5uM). Reported to exhibit good aqueous solubility (>100uM at pH 7.4) and inhibit the proliferation (IC50=17uM) and cellular eIF4E Ser209 phosphorylation (IC50=4.7uM) of MV4:11 cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N? 2HCl. US Biological Life Sciences. | Worldwide |
mTOR Inhibitor XI, Torin1 (1- (4- (4-propionylpiperazin-1-yl) -3- (trifluoromethyl) phenyl) -9- (quinolin-3-yl) benzo[h][1, 6]naphthyridin-2 (1H) -one, DNA-PK Inhibitor VI, PI 3-K Inhibitor XVIII) Quick inquiry Where to buy Suppliers range | A cell-permeable pyridinonequinoline derivative that acts as a highly potent, ATP-competitive inhibibitor against mTOR and DNA-PK (IC50 = 4.32 and 6.34nM, respectively), while inhibiting PI 3-K only at much higher concentrations (IC50 =171 to 533nM). Effectively inhibits mTORC1-mediated S6K1 phosphorylation in MEF (IC50 = 2nM) in vitro, as well as mTORC2-mediated Akt and mTORC1-dependent S6 phosphorylations in murine lung and liver in vivo (up to 6h post single 20mg/kg i.p. dose). Despite its poor in vivo stability (T1/2 = 4.52h in mice; 10mg/kg i.p.), Torin1 is reported to completely suppress U87MG-derived tumor expansion in mice when administered via daily i.p. at a high dosage of 200mg/kg. Also reported to effectively inhibit cellular mTORC1 functionalities known to be rapamycin-resistant. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
PRL-3 Inhibitor (BR-1, P0108, Phosphatase of Regenerating Liver 3 Inhibitor, PTP4A3 Inhibitor) Quick inquiry Where to buy Suppliers range | Phosphatase of regenerating liver 3 (PRL-3, also known as PTP4A3) plays critical roles in cell proliferation, motility, and invasion, and thus contributes to cancer metastasis. PRL-3 inhibitor is a cell-permeable benzylidene rhodamine that inhibits PRL-3 (IC50=900nM for human PRL-3 in vitro), with minimal activity against other phosphatases. It reduces the invasion of mouse melanoma B16F10 cells in a cell-based assay. PRL-3 inhibitor has been used to elucidate the actions of this enzyme, demonstrating that it dephosphorylates Tyr783 on integrin beta1 and modulates VEGF-mediated endothelial cell migration. It dose-dependently inhibits the growth and triggers apoptosis in cancer cell lines. Group: Biochemicals. Alternative Names: 5-[[5-bromo-2-[(2-bromophenyl) methoxy] phenyl] methylene] -2- thioxo-4-thiazolidinone. Grades: Highly Purified. CAS No. 893449-38-2. Pack Sizes: 1mg, 5mg, 10mg, 25mg. Molecular Formula: C17H11Br2NO2S2. US Biological Life Sciences. | Worldwide |
Sphingosine Kinase Inhibitor IV, CB5468139 (N-(3-chloro-1,4-dioxo-1,4-dihydro-2-naphthalenyl)-N-cyclohexylacetamide, SK Inhibitor IV, Sphingosine Kinase Inhibitor IV) Quick inquiry Where to buy Suppliers range | A cell-permeable naphthoquinone derivative that acts as an ATP-competitive inhibitior against sphingosine kinase 1 (IC50 = 2uM; [sphingosine] = 10uM & [ATP] = 100uM) and several protein kinases, including, but not limited to, TNK2, AURKB, Met, Syk, AURKC, Fyn, Flt2, PIM2, MST2, CLK1, Tie1, and Fak (IC50 <2uM), while exhibiting much reduced potency toward DAG Kinase and sphingosine kinase 2 (37% and no inhibition, respectively, at 100uM). Shown to be more potent than SK1/2 dual inhibitor against kidney adenocarcinoma A498 proliferation (GI50 = 10 and 20uM, respectively; 48h) and the two inhibitors are also reported to induce differential modulations of A498 cellular ceramides and S1P levels when applied at their respective GI50. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
sPLA2-IIA Inhibitor II, KH064 ( (S) -5- (4- (benzyloxy) phenyl) -4- (7-phenylheptanamido) pentanoic Acid, Phospholipase A2 Group IIA Inhibitor II, PLA2g2a Inhibitor II) Quick inquiry Where to buy Suppliers range | A reversible, potent, and selective sPLA2-IIA/PLA2g2a (phospholipase A2 group IIA) inhibitor (IC50 = 29nM) that displays much reduced potency against sPLA2-V/PLA2g5 (PLA2 group V; IC50 = 2uM) and is reported not to affect the activity of cytosolic cPLA2, Ca2+-independent iPLA2, 30 human GPCRs, and 25 other enzymes. In addition to being useful in studying PLA2g2a-mediated cellular responses in cultures in vitro (100% inhibition of LPS-induced PGE2 production in HMC-1 cells; 15 min 10uM pretreatment), KH064 is orally available in rats and efficacious in various rat disease models in vivo (5mg/kg p.o.), including adjuvant-induced arthritis, spontaneous hypertension, high fat diet-induced metabolic disorders. Comparing to the substrate-competitive inhibitor c(2NapA)LS(2NapA)R, KH064 also effectively chelates sPLA2-IIA active site Ca2+ in addition to targeting the enzyme's N-terminal lipid substrate binding site. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Survivin Inhibitor, YM155 (Survivin Inhibitor I, Interleukin Enhancer-Binding Factor 3 Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable imidazolium derivative that suppresses survivin expression, blocks survivin promoter activity, and induces apoptosis in a variety of tumor cell lines (IC50 = 540nM) in a dose-dependent manner. The main target of YM155 appears to be the interleukin enhancer-binding factor 3 (ILF3/NF110) with shorter C-terminal lengths associated with reduced binding. Exhibits potent anti-tumor effects without any severe systemic toxicity in murine models. Reported to induce tumor regression by suppressing intratumor survivin levels in PC3-xenograph tumor models (by 47% and 80% at 1 and 5mg/kg, respectively. Group: Biochemicals. Grades: Highly Purified. CAS No. 781661-94-7. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Tankyrase1/2 Inhibitor III (TNKS1/2 Inhibitor III, Wnt Pathway Inhibitor XIV, 3-(4-Methoxyphenyl)-5-((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-ylthio)methyl)-1,2,4-oxadiazole) Quick inquiry Where to buy Suppliers range | A cell-permeable triazolylthiomethyl-oxadiazole compound that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (=79 and 28nM, respectively), and acts as a potent and reversible TNKS1/2 dual inhibitor (IC50=33nM TNKS2 in an auto-PARsylation assay). Shown to interact with the adenosine diphosphate linker portion of the NAD+ donor site, and display excellent selectivity over PARP1 and PARP2 activities (IC50>19uM); stabilize Axin2 levels (EC50=709nM in SW480 cells), and antagonize Wnt signaling (IC50=215nM in HEK293-SuperTopFlash assay). Exhibits minimal activity towards cytochrome P450 enzymes (IC50=21 and 5.7uM for CYP2C9 and CYP3A4) and hERG ion channel (IC50>30uM), and adequate microsomal stability. Group: Biochemicals. Grades: Highly Purified. CAS No. 865565-29-4. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Tie2/Trk Dual Inhibitor (Tie2 Inhibitor IV, Trk Inhibitor VII) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC50 = 40 and 0.4nM, respectively; [ATP] = 100uM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC50 = 3.7 and 4nM, with respective NIH 3T3 transfectant), displaying much reduced potency against PDGFR (IC50 =1.4uM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >10uM). Reported to be efficacious in suppressing rat C6 glioblastoma tumor expansion (10 to 33mg/kg/d, or 10mg/kg/12h p.o.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?O?, Primary Target: TrkA. US Biological Life Sciences. | Worldwide |
TNP-470 (AGM-1470, O-(Chloroacetyl-carbamoyl)fumagillol, AGM1470, MetAP-2 Inhibitor II, MetAP2 Inhibitor II, Methionine Aminopeptidase 2 Inhibitor II, TNP470) Quick inquiry Where to buy Suppliers range | A cell-permeable Fumagillin analog that inhibits MetAP2, but not MetAP1, methionine aminopeptidase activity (IC50 = 1nM against human MetAP2), without affecting the inhibitory activity of MetAP2 against HRI- (heme-regulated inhibitor kinase) catalyzed eIF-2alpha phosphorylation. A potent endothelial cytostasis inducer (IC50 = 25 pM and 37 pM, respectively, against HUVEC and bovine BAEC) in vitro and an effective anti-angiogenesis agent in vivo (2-100mg/kg in mice and rats; s.c.). Group: Biochemicals. Grades: Highly Purified. CAS No. 129298-91-5. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
USP14 Inhibitor, IU1 (1-(1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone, 1-(1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl)-2-pyrrolidin-1-ylethanone, Ubiquitin Specific Protease 14 Inhibitor, DUB Inhibitor IX) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrrolylpyrrolidinyl-ethanone compound that directly targets proteasome-associated DUB (deubiquitinating enzyme) USP14 and acts as a potent, active-site-directed and reversible inhibitor of hUSP14 deubiquitinating catalytic activity (IC50=4.7uM for Ub-AMC hydrolysis) with excellent selectivity over proteasome-free USP14 and 8-other hDUBs including IsoT (IC50=100uM), UCH37, BAP1, UCH-L1, UCH-L3, USP15, USP2 and USP7 (IC50>700uM). Shown to enhance proteolysis in cells and induce degradation of misfolded toxic proteins like tau, TDP-43 and GFAP (glial fibrillary acidic protein) in coexpressed-wtMEFs at 50uM and offer protection against oxidative stress-induced cytotoxicity. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
VEGFR2 Kinase Inhibitor VII, SKLB1002 (VEGFR Tyrosine Kinase Inhibitor XXXV, 6,7-Dimethoxy-4-(5-methyl-1,3,4-thiadiazol-2-ylthio)quinazoline, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor VII) Quick inquiry Where to buy Suppliers range | A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50=32nM), while exhibiting much reduced or little activity against 16 other kinases. An effective antiangiogenesis agent (98% inhibition of HUVEC tube formation at 10uM; 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5uM) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days; 100mg/kg/day; i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
17b-Hydroxysteroid Dehydrogenase Type-3 Inhibitor (17b-HSD3 Inhibitor, 5-(3-Bromo-4-hydroxybenzylidene)-3-(4-methoxyphenyl)-2-thioxothiazolidin-4-one) Quick inquiry Where to buy Suppliers range | A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of testosterone by directly inhibiting 17b-HSD3- (17b-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of delta4-dione C17 ketone in a delta4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50=0.6, 6.0, and 40nM, respectively, against momoset, human, and mouse 17b-HSD3 activity in testes homogenate), and selective manner, displaying no activity against 17b-HSD1 and 17b-HSD2 activity. Poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
3,3'-Diamino-4'-methoxyflavone, DD1 (3-amino-2-(3-amino-4-methoxyphenyl)-4H-chromen-4-one, p76S6 Inhibitor, DD1, Proteasome Inhibitor, DD1) Quick inquiry Where to buy Suppliers range | A cell-permeable flavone derivative that arrests the proliferation of acute myeloid leukemia cells (NB4, U937, HL-60, OCI AML3), in a dose and time-dependent manner (optimum at ~20uM and 96h) and blocks the colony formation in samples from acute myeloid leukemia patients, without affecting normal blood cells. Shown to reduce mitochondrial membrane potential and Bad phosphorylation (at Ser136), induce Bax and caspase 3, 8, and 9 activation in U937 cells. Does not affect the phosphorylation of Akt1, but significantly reduces the expression and phosphorylation of p70S6 kinase in U937 cells. Reported to inhibit the chymotrypsin-like activity of proteasome (IC50 = 2.0uM) and this effect is synergistic with bortezomib. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Ack1 Inhibitor, AIM-100 (Activated Cdc42 Kinase 1 Inhibitor, (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine) Quick inquiry Where to buy Suppliers range | A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72h 8uM) and in castrated mice in vivo (4mg/kg/96h injections on day 7/11/15/19/23/27 post tumor transplant). Group: Biochemicals. Grades: Highly Purified. CAS No. 873305-35-2. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Adenovirus Proteinase Inhibitor, NSC 37249 (2- (Dicyclohexylamino) -N- (4- (4- ( (2- (dicyclohexylamino) acetyl) amino) phenyl) sulfonylphenyl) acetamide, N, N?- (Sulfonyldi-4, 1-phenylene) bis (2- (dicyclohexylamino) acetamide, AVP Inhibitor) Quick inquiry Where to buy Suppliers range | A sulfonyl diphenyl ene -bis-dicyclohexyl aminoacetamide compound that acts as a potent and selective inhibitor against adenovirus cysteine proteinase AVP by targeting simultaneously AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket (Ki = 150nM) and AVP-pVIc substrate-binding site (Ki = 400nM), blocking both AVP-pVIc active complex formation (IC50 = 140nM; [substrate] = 5uM & [pVIc] = 40uM) and catalytic activity (IC50 = 490nM; [substrate] = 5uM) without affecting trypsin or papain protease activity even at concentrations as high as 10uM. Group: Biochemicals. Grades: Purified. CAS No. 2907-88-2. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences. | Worldwide |
AMPK Inhibitor, Compound C (6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine, Dorsomorphin, BMP Inhibitor I) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50=25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFbR-I, ZAPK, Syk, PKCth, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100=2.5uM) and VEGF signaling-dependent intersomitic vessel formation (EC50=5uM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR and/or Metformin for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. CAS Number:866405-64-3. Group: Biochemicals. Grades: Highly Purified. CAS No. 866405-64-3. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C??H??N?O. US Biological Life Sciences. | Worldwide |
ATR Inhibitor IV (VE821, 3-amino-6- (4- (methylsulfonyl) phenyl) -N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV) Quick inquiry Where to buy Suppliers range | A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13nM; IC50/[ATP] = 70nM/50uM and 128nM/100uM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1uM, respectively, against DNA-PK, PI 3-K-gamma, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10uM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24h) VE-821 treatment, either alone or in synergy with Cisplatin, results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72h) in cultures with ATM-p53 pathway defects.CAS No.1232410-49-10. Group: Biochemicals. Grades: Highly Purified. CAS No. 1232410-49-10. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences. | Worldwide |
Autotaxin Inhibitor III, PF-8380 (Atx Inhibitor III, PF-8380, 6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one) Quick inquiry Where to buy Suppliers range | An orally bioavailable piperazinyl benzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50=2.8 and 1.7nM for recombinant human enzyme-b isoform employing FS-3 and LPC (lysophosphatidyl choline) as substrates, respectively; 1.16 and 1.15nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30mg/kg, p.o.).CAS No:1144035-53-9. Group: Biochemicals. Grades: Highly Purified. CAS No. 1144035-53-9. Pack Sizes: 10mg. Molecular Formula: C??H??Cl?N?O?. US Biological Life Sciences. | Worldwide |
b-Catenin/Tcf Inhibitor II, PKF118-310 (1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor IV) Quick inquiry Where to buy Suppliers range | A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts b-catenin-Tcf4 interaction (IC50=0.8uM in cell-free binding assays) and inhibits b-catenin-regulated cellular transcription activity (IC50=0.3uM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse b-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of b-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
b-Catenin/Tcf Inhibitor V, BC21 (Copper, di-u-chlorobis[1-[(1-piperidinyl-kN)methyl]-2-naphthalenolato-kO]di-(9Cl), Wnt Pathway Inhibitor XV) Quick inquiry Where to buy Suppliers range | A cell-permeable dimeric copper complex that competitively binds b-catenin and disrupts b-catenin/Tcf4 interaction reversibly (IC50=5.0uM), and acts as a Wnt signaling inhibitor. Shown to induce preferential growth arrest in b-catenin overexpressing HCT116 colon cancer and HEK293 cells (≤10uM), and downregulate mRNA expressions of c-Myc and cyclin D1. Reported to inhibit PP2C and proteasomal activities at higher concentrations (~50uM). Group: Biochemicals. Grades: Highly Purified. CAS No. 691005-38-6. Pack Sizes: 10mg. Molecular Formula: C32H36Cl2Cu2N2O2, Molecular Weight: 678.6. US Biological Life Sciences. | Worldwide |
CaMKII Inhibitor XII (Ca2+/Calmodulin-Dependent Protein Kinase II Inhibitor XII) Quick inquiry Where to buy Suppliers range | A pyrimidinyl sulfonamide compound that acts as a potent, reversible and CaM non-competitive inhibitor of CaMKII activities (IC50 = 0.063uM) with excellent selectivity over several kinases (IC50 = >60, 36, 11, 30 and 21uM for CaMKIV, MLCK, p38alpha, Akt1 and PKC, respectively). Shown to exhibit ~25-fold greater potency towards CaMKII than the CaM-competitive inhibitor KN-93. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
Carbonic Anhydrase IX/XII Inhibitor (CAIX Inhibitor) Quick inquiry Where to buy Suppliers range | A cell permeable benzenesulfonamide Carbonic Anhydrase (CA) inhibitor that is selective for human hCA IX and hCA XII (Ki = 0.9nM and 5.7nM, respectively) against two other physiologically relevant hCA isoforms (Ki = 23.4nM and 15nM for hCA I and hCA II, respectively), as compared with another CA inhibitor AAZ (Ki = 250nM, 12nM, 25nM, and 5.7nM for hCA I, hCA II, hCA IX, and hCA XII, respectively). It is shown to effectively inhibit the formation of metastases by 4T1 breast cancer cells in a mouse model dose-dependently at pharmacologic concentrations of 15-45mg/kg. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
Carbonic Anhydrase IX/XII Inhibitor II, U-104 (CAIX Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell permeable ureido-sulfonamide Carbonic Anhydrase (CA) inhibitor that is selective for human hCA IX and hCA XII (KiEnM and 4.5nM, respectively) against two other physiologically relevant hCA isoforms (KiP80nM and 9640nM for hCA I and hCA II, respectively). It elicits anti-tumor growth effects dose-dependently from 19 to 38mg/kg in a mouse tumor growth model implanted with MDA-MB-231 LM2-4Luc+ cells, and demonstrates metastasis inhibition in a mouse metastasis model injected with 4T1 cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
Casein Kinase I Inhibitor III, PF-4800567 (CKI Inhibitor III, PF-4800567)(3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrazolopyrimidinyl amino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKle with ~22-fold greater potency over CKld (IC50=32 and 711nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1uM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKle cells over CKld-transfected cells (IC50=0.13 and 2.65uM, respectively), and PER2 degradation in COS7-GFP-PER2-CKle cells. Unlike Casein Kinase I Inhibitor II, PF-670462, PF-4800567 exerts only marginal effect on circadian clock under similar conditions. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
CBF beta-Runx1 Inhibitor II, Ro5-3335 ([7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFalpha-CBFbeta Inhibitor II) Quick inquiry Where to buy Suppliers range | A cell-permeable benzodiazepine that suppresses CBFalpha/Runx1-CBFbeta transactivation activity (25uM; 293-0 cells) via direct bindings to both subunits of the heterodimeric transcription factor complex. Shown to inhibit oncogenic fusion CBFB-MYH11-, TEL-RUNX1-, and RUNX1-ETO-, dependent leukemia cells proliferation (IC50 = 1.1 to 21.7uM) in vitro and more effectively reduce peripheral blood c-kit+ population (300mg/kg/d via animal feed) than Cytarabine in a murine Cbfb-MYH11 leukemia model in vivo. Comparing to CBFbeta-Runx1 Inhibitor I, Ro5-3335 modulates the Runx1-CBFbeta heterodimer formation without completely disrupting the subunits interaction. Group: Biochemicals. Grades: Highly Purified. CAS No. 30195-30-3. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Cdc25 Inhibitor IV, NSC 95397 (2,3-Bis(2-hydroxyethylthio)-1,4-naphthalenedione, PTP Inhibitor XXIX) Quick inquiry Where to buy Suppliers range | A cell-permeable, para-naphthoquinone that has been reported to inhibit protein tyrosine phosphatase activity, including Cdc25 dual specificity phosphatase (Ki=32nM, 96nM, and 40nM for Cdc25A, -B, and -C, respectively) and blocks G2M transition in murine carcinoma cells. In addition, it is shown to inhibit S100A4 binding to myosin-IIA via covalent modification of cysteine residues, Cys81 and Cys86, in the target binding cleft (IC50=1.8uM). It demonstrates inhibitory activity against S100A4-mediated depolymerization of myosin-IIA filaments. Group: Biochemicals. Grades: Highly Purified. CAS No. 93718-83-3. Pack Sizes: 10mg. Molecular Formula: C??H??O?S?, Molecular Weight: 310.4. US Biological Life Sciences. | Worldwide |
Cytoplasmic Dynein Inhibitor, Ciliobrevin D (2- (7-chloro-4-oxo-3, 4-dihydroquinazolin-2 (1H)-ylidene)-3- (2, 4-dichlorophenyl)-3-oxopropanenitrile) (AAA+ ATPase Motor Cytoplasmic Dynein Inhibitor) Quick inquiry Where to buy Suppliers range | A cell-permeable benzoyl dihydroquinazolinone derivative that acts as a reversible and specific blocker of AAA+ ATPase motor cytoplasmic dynein and disrupts spindle pole focusing, cold-stable microtubule formation, kinetochore-microtubule attachment, and melanosome aggregation in a dose-dependent manner (~10-40uM). Shown to perturb protein trafficking within the primary cilia and cause a significant increase in intraflagellar transport protein 88 (IFT88) levels at the distal tip of primary cilia. Reported to disrupt primary cilium-dependent Gli regulation and block Hedgehog signaling. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
D-Amino Acid Oxidase Inhibitor III, AS057278 (5-methyl-1H-pyrazole-3-carboxylic Acid, DAAO Inhibitor III) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrazolocarboxylic acid that acts as a selective D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) inhibitor (IC50 = 910nM against human DAO; [D-ser] = 10mM) and effectively protects DAO overexpressing cultures from oxidative stress-induced cell death upon D-Ser (50mM) exposure (ED50 ≤3.95uM), while exhibiting little affinity toward nMDAR glycine binding site or inhibitory activity against D-aspartate oxidase (DDO/DSOX). Reported to be orally available and blood-brain barrier-permeant in rats and effectively prevent PCP (phencyclidine) from suppressing PPI (prepulse inhibition) response in mice (single 80mg/kg or 56X 20mg/kg/12h b.i.d. oral dosages) in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 402-61-9. Pack Sizes: 50mg. US Biological Life Sciences. | Worldwide |
DNA Methyltransferase Inhibitor V, RSC133 (DNA MTase Inhibitor V, (E) -3- (3- (1H-Indol-3-yl) acrylamido) benzamide, ID133, iPSC Induction Enhancer III, Reprogramming Stimulating Compound 133) Quick inquiry Where to buy Suppliers range | A cell-permeable indolylacrylamido-benzamide compound that is reported to target Dnmt1 at the cofactor SAM-binding site and enhance the efficiency of iPSC production from both murine MEF (10uM starting 5 d post KSOM viral infection) and human foreskin fibroblast (10uM starting same day as or 5 d post KSOM viral infection) cultures with accompanying cellular Dnmt1 activity reduction, affecting hFF viability only at high concentrations (78% of control post 72h 100uM treatment). Also shown to help maintain H9 hESCs in undifferentiated state when cultured in unconditioned media (10uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. Molecular Formula: C??H??N?O?, Primary Target: Dnmt1. US Biological Life Sciences. | Worldwide |
eEF2K Inhibitor, A-484954 (7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide, Eukaryotic Elongation Factor-2 Kinase Inhibitor, A-484954) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrido-pyrimidinedione derivative that acts as a highly potent and selective inhibitor of eukaryotic elongation factor-2 kinase (eEF2K) (IC50=280nM). Exhibits very little activity against a broad panel of serine/threonine and protein tyrosine kinases. Inhibits eEF2 phosphorylation in multiple cell lines tested without affecting the net eEF2 levels. At concentration where it inhibits eEF2K activity, it has no effect on the proliferation of cancer cell lines.CAS No.142557-61-7. Group: Biochemicals. Grades: Highly Purified. CAS No. 142557-61-7. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?, Molecular Weight: 289.3. US Biological Life Sciences. | Worldwide |
ERO1 Inhibitor I, Erodoxin (Endoplasmic Reticulum Oxidase 1 Inhibitor, 1-Bromo-5-methoxy-2,4-dinitrobenzene) Quick inquiry Where to buy Suppliers range | A cell-permeable dinitrobromobenzene compound that acts as a selective inhibitor of yeast Endoplasmic Reticulum Oxidase 1 (ERO1), but has somewhat weaker activity against mouse ERO1a (IC50=400uM). Predicted to form thiol adducts and inhibits ERO1-dependent oxidation of thioredoxin-1 (Trx1) activity in vitro. Shown to cluster with genes involved in protein folding, glycosylation and cell wall biosynthesis, and delay carboxypeptidase Y (CPY) processing to the vacuolar form in wt-yeast cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. Molecular Formula: C?H?BrN?O?, Molecular Weight: 277. US Biological Life Sciences. | Worldwide |