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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.
14-3-3η Protein inhibitor 1
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a K D of 35 μM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2770842-10-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-146302.
15-Lipoxygenase Inhibitor 1
15-Lipoxygenases (15-LO) inhibitor 1 is a heterocyclic pyrimidobenzothiazine compound that inhibits 15-LO with an IC50 value of 18 μM. Synonyms: 15-LO Inhibitor 1; 4-methyl-2-(4-methylpiperazin-1-yl)-5H-pyrimido[4,5-b][1,4]benzothiazine. Grades: ≥95%. CAS No. 928853-86-5. Molecular formula: C16H19N5S. Mole weight: 313.4.
A cell-permeable, thiazolidinedione derivative that acts as a 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor (IC50=25nM). It is shown to increase PGE2 levels in IL-1b-stimulated A549 cells, dose-dependently, in the range of 0-20uM, and elicits cochlear blood flow (CBF) increase by 15% and 55% when applied intravenously to 250g guinea pigs at 10ug and 20ug respectively. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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.
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187-1, N-WASP inhibitor
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC 50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein [1] [2]. Uses: Scientific research. Group: Peptides. CAS No. 380488-27-7. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P1045.
187-1, N-WASP inhibitor
187-1, N-WASP inhibitor can inhibit neural Wiskott-Aldrich syndrome protein by stabilizing the autoinhibited state of the protein. It can also block phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly with an IC50 value of~ 2 μM. Synonyms: n-wasp-inhibitor,187-1; cyclo[Gln-Lys-D-Phe-D-Pro-D-Phe-Phe-D-Pro-Gln-Lys-D-Phe-D-Pro-D-Phe-Phe-D-Pro]; cyclo[L-glutaminyl-L-lysyl-D-phenylalanyl-D-prolyl-D-phenylalanyl-L-phenylalanyl-D-prolyl-L-glutaminyl-L-lysyl-D-phenylalanyl-D-prolyl-D-phenylalanyl-L-phenylalanyl-D-prolyl]. Grades: >98%. CAS No. 380488-27-7. Molecular formula: C96H122N18O16. Mole weight: 1784.13.
187-1, N-WASP inhibitor
Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 uM) but does not directly inhibit actin polymerization. Group: Biochemicals. Grades: Highly Purified. CAS No. 380488-27-7. Pack Sizes: 1mg. Molecular Formula: C96H122N18O16, Sequence: US Biological Life Sciences.
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187-1, N-WASP INHIBITOR
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein. Uses: Designed for use in research and industrial production. Additional or Alternative Names: CYCLO(LKDFDPDFLFDPLQ)2;187-1, N-WASP INHIBITOR;N-WASP-INHIBITOR, 187-1;M.W. 1784.13 C96H122N18O16. Product Category: Inhibitors. Appearance: Solid. CAS No. 380488-27-7. Molecular formula: C96H122N18O16. Mole weight: 1784.11. Purity: 0.96. IUPACName: 187-1, N-WASP inhibitor. Canonical SMILES: C1CC2C(=O)NC(C(=O)NC(C(=O)N3CCCC3C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)NC(C(=O)NC(C(=O)N5CCCC5C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2C1)CC6=CC=CC=C6)CCCCN)CCC(=O)N)CC7=CC=CC=C7)CC8=CC=CC=C8)CC9=CC=CC=C9)CCCCN)CCC(=O)N)CC1=CC=CC=C1)CC1=CC=CC=C1. Product ID: ACM380488277. Alfa Chemistry ISO 9001:2015 Certified.
2,4-Dibenzyl-5-oxothiadiazolidine-3-thione (GSK-3ß Inhibitor III. )
Melting Point: 104-107°C. Group: Biochemicals. Alternative Names: GSK-3ß Inhibitor III. Grades: Highly Purified. CAS No. 72966-20-2. Pack Sizes: 5mg. US Biological Life Sciences.
2-Methacryloxyethyl D-glucopyranoside - 25-50% in an aqueous solution containing 200 ppm MEHQ inhibitor is a cutting-edge biomaterial utilized in advanced pharmaceutical release matrices and encapsulation methodologies. This aqueous formulation serving as an indispensable tool for precise and site-specific administration of therapeutic compounds, applied in research of a wide spectrum of ailments such as diabetes, cancer, and cardiovascular maladies. Synonyms: 2-Methacryloxyethyl D-glucopyranoside; GEMA; 2-[(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyethyl 2-methylprop-2-enoate; 132153-84-5; 2-methacryloxyethyl glucoside; glucosyloxyethyl methacrylate; SCHEMBL222100; DTXSID30927559; 2-(Hexopyranosyloxy)ethyl 2-methylprop-2-enoate; J-006131; D-GLUCOPYRANOSIDE,2-[(2-METHYL-1-OXO-2-PROPEN-1-YL)OXY]ETHYL; 2-(((3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)ethyl methacrylate; 2-((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yloxy)ethyl methacrylate. CAS No. 132153-62-9. Molecular formula: C12H20O8. Mole weight: 292.3.
[2- (Methacryloyloxy) ethyl]trimethylammonium chloride solution, 75 wt. % in H2O, contains 600 ppm MEHQ as inhibitor
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.
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4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (GSK-3ß Inhibitor I, TDZD-8)
Glycogen Synthase Kinase-3ß is a highly conserved ubiquitously expressed serine/threonine protein kinase involved in signal transduction cascades of multiple cellular processes. 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione, also known as TDZD-8, is a thiadiazolidinone (TDZD) analogue that acts as a highly selective, non-ATP competitive inhibitor of GSK3b (IC50 =2nM). It binds to the active site of GSK3b. It does not significantly affect the activities of Cdk-1/cyclin B, CK-II, PKA, and PKC (IC50 >100nM). Group: Biochemicals. Alternative Names: GSK-3ß Inhibitor I, TDZD-8. Grades: Highly Purified. CAS No. 327036-89-5. Pack Sizes: 10mg. US Biological Life Sciences.
A cell permeable hydroxytricyclic derivative that acts as a specific and reversible inhibitor of transient receptor potential melastatin 4 (TRPM4) (IC50=20uM in HEK293 cells). Does not affect TRPM5 and cystic fibrosis transmembrane conductance regulators (CFTR) channels. Decreases the occurrence of early after depolarizations (EAD) and exhibits an anti-arrhythmic effect that is independent of the action of protein kinase A. Shown to abolish nMDA-induced burst firing in dopaminergic neurons. Does not affect K+ currents at ~10uM, but at higher concentration (~100uM) it reversibly reduces K+ currents. Group: Biochemicals. Grades: Highly Purified. CAS No. 484-17-3. Pack Sizes: 50mg. US Biological Life Sciences.
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a-Amylase Inhibitor
a-Amylase Inhibitor. Product ID: 9-02347. Purity: a:b anomeric ratio 1:2.3.
Cell-permeable. A potent and selective inhibitor of ACC2 (Acetyl-CoA Carboxylase) (IC50 = 28nM for hACC2 vs 210nM for hACC1 in in vitro studies). Group: Biochemicals. Alternative Names: N-(1-(2-(4-Isopropoxyphenoxy)-2,5-bithiazol-5-yl)ethyl)acetamide. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
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Ac-CoA Synthase Inhibitor 1
Ac-CoA Synthase Inhibitor 1 is an anti-virus agent. Synonyms: 1-(2,3-Di(thiophen-2-yl)quinoxalin-6-yl)-3-(2-methoxyethyl)urea. Grades: ≥95%. CAS No. 508186-14-9. Molecular formula: C20H18N4O2S2. Mole weight: 410.51.
Acidic Mammalian Chitinase Inhibitor, Bisdionin F
A cell-permeable, competitive Acidic Mammalian Chitinase (AMCase) Inhibitor (IC50=0.92uM and Ki=0.42uM for hAMCase, and IC50=2.2uM for mAMCase, in vitro) that demonstrates 20-fold selectivity for hAMCase over hCHIT1. It is shown to decrease chitinase enzymatic activity (5mg/kg, i.p.) in the lungs of control PBS- and OVA-challenged mice. Furthermore, it attenuates lung chitinase activity, reduces eosinophil influx, and improves ventilatory function, in vivo, in a murine model of allergic inflammation. It also causes neutrophilia in the lungs of OVA-challenged mice. Group: Biochemicals. Alternative Names: AMCase Inhibitor, 3,7-dimethyl-1-(3-(3-methyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl)propyl)-1H-purine-2,6(3H,7H)-dione. Grades: Highly Purified. CAS No. 917877-86-2. Pack Sizes: 5mg. US Biological Life Sciences.
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.
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ADAMTS-5 inhibitor
ADAMTS-5 (A Disintegrin And Metalloproteinase with ThromboSpondin motifs 5) is an aggrecanase-2. ADAMTS-5 is involved in the catabolism of aggrecan and collagen in the articular cartilage matrix during Osteoarthritis (OA). Synonyms: ADAMTS-5 Inhibitor; ADAMTS 5 Inhibitor; ADAMTS5 Inhibitor; 5-[[5-[(4-chlorophenyl)methylsulfanyl]-1-methyl-3-(trifluoromethyl)pyrazol-4-yl]methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one. Grades: 99%. CAS No. 929634-33-3. Molecular formula: C16H11ClF3N3OS3. Mole weight: 449.92.
ADAMTS-5 Inhibitor
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC 50 of 1.1 μM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 929634-33-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-114996.
ADAR1, Inhibitor Peptide (Adenosine Deaminases Acting on RNA 1)
The mammalian Adenosine Deaminases Acting on RNA (ADAR) constitute a family of sequence-related proteins involved in pre-mRNA editing of nuclear transcripts through site-speci?c adenosine modi?cation. ADARs are not active on adenosine-mononucleotide and are only distantly related by sequence to adenosine and AMP deaminases involved in purine metabolism. The ADARs convert certain adenosine bases in an RNA transcript into inosines by removing an amino group involved in Watson-Crick base pairing. The ADARs recognize a double stranded RNA (dsRNA) structure in the transcript that is formed between the editing site complementary sequence (ECS), usually located in the downstream 3 intron of the transcript, and the sequence to be edited. Group: Molecular Biology. Grades: Purified. Pack Sizes: 100ug. US Biological Life Sciences.
A cell-permeable and reversible inhibitor of protein kinase A (Ki = 11uM). Resistant to hydrolysis by phosphodiesterases. Noncompetitive with respect to ATP. Group: Biochemicals. Grades: Highly Purified. CAS No. 151837-09-1. Pack Sizes: 5umol. US Biological Life Sciences.
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Adenosine receptor inhibitor 1
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with K i values of >1000, 68.5, >1000, >1000 nM for A 1 AR, A 2A AR, A 2B AR, A 3 AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2550400-52-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg. Product ID: HY-147907.
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.
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AKR1C1 Inhibitor, 5-PBSA
A cell-permeable salicylic acid compound that acts as a highly potent, active-site directed and substrate competitive AKR1C1 inhibitor (Ki=4nM) with moderate to excellent selectivity over AKR1C2, AKR1C3 and AKR1C4 (Ki=0.087, 4.2 and 18.2uM, respectively). Shown to inhibit the metabolism of progesterone by AKR1C1 (IC50=460nM in AKR1C1 overexpressing BAECs).CAS No.4906-68-7. Group: Biochemicals. Alternative Names: Aldo-Keto Reductase family 1 member C1 Inhibitor, 5-PBSA, 3-Bromo-5-phenylsalicylic acid, 20α-Hydroxysteroid Dehydrogenase Inhibitor, 5-PBSA. Grades: Highly Purified. CAS No. 4906-68-7. Pack Sizes: 25mg. Molecular Formula: C??H?BrO?. US Biological Life Sciences.
A cell-permeable 3-phenyl-aminobenzoate compound that acts as a potent, competitive, reversible, active-site targeting inhibitor of aldo-keto reductase 1C3 (AKR1C3; type 5 17b-hydroxysteroid dehydrogenase) (IC50 = 60nM) with excellent selectivity over other closely related human AKR isoforms (IC50 = 22.7, 15.4, 62.7, >50, and >50uM for and AKR1C1, AKR1C2, AKR1C4, AKR1B1 and AKR1B10, respectively. Exhibits a weak inhibitory effect on cyclooxygenase 1 and 2 (IC50 = 100uM). Shown to efficiently block the AKR1C3-mediated production of testosterone in LNCaP-AKR1C3 cells (~10uM). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
Cell-permeable. A potent and selective inhibitor of Akt1/Akt2 activity (IC?? = 58nM (Akt1), 210nM (Akt2) and 2.12uM (Akt3) in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations (50uM). Group: Biochemicals. Grades: Highly Purified. CAS No. 612847-09-3. Pack Sizes: 1mg. US Biological Life Sciences.
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Akt Inhibitor IV
Akt inhibitor IV is an inhibitor of Akt activation that inhibits Akt-mediated nuclear export of Forkhead box class O transcription factor 1a (FOXO1a; IC50 = 625 nM) and reduces phosphorylation of Akt at Ser473 and Thr308 in a dose-dependent manner. Synonyms: 5-(2-Benzothiazolyl)-3-ethyl-2-[2-(methylphenylamino)ethenyl]-1-phenyl-1H-benzimidazolium iodide. Grades: ≥95%. CAS No. 681281-88-9. Molecular formula: C31H27N4S·I. Mole weight: 614.6.
AKT inhibitor IV
Akt inhibitor-IV (AKTIV) acts as a PI3K-Akt inhibitor at the E isomer (HY-14971), with potent cytotoxicity [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AKTIV. CAS No. 681281-88-9. Pack Sizes: 1 mg. Product ID: HY-14971A.
AKT inhibitor VIII
Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity. It does not exhibit any inhibitory effect against pleckstrin homology (PH) domain-lacking Akts, AGC family kinases, PKA, PKC or SGK. It also prevails over Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and has been shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 in cultured cells and in mice. Synonyms: AKT inhibitor VIII; AKT-inhibitor-VIII; AKT inhibitor-8; AKT-inhibitor-8; Akt-I 1,2; Akti-1/2. Sigma-A6730. 2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-. Grades: >98%. CAS No. 612847-09-3. Molecular formula: C34H29N7O. Mole weight: 551.64.
A cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50=58nM, 210nM, and 2.12uM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50uM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation / activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 612847-09-3. Pack Sizes: 1mg, 5mg. US Biological Life Sciences.
A cell-permeable chloroacetyl-indole compound that inhibits Akt1 and Akt2 kinase activity (IC50 <1uM) by directly targeting Akt PH domain, exhibiting little or much reduced activity against a panel of 84 other kinases. Effectively inhibits Akt-mediated downstream effector proteins phosphorylation in a time-dependent manner, resulting in effective apoptosis induction in HCT116 and HT29 cultures (by 55% and 60%, respectively; 4uM for 4 days). Reported to retard HCT116-derived tumor growth in mice (EC50=30mg/kg; 5 times/wk for 3 wks via p.o.) in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 28755-03-5. Pack Sizes: 25mg. US Biological Life Sciences.
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.
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AKT Kinase Inhibitor
AKT Kinase Inhibitor is a Akt Kinase Inhibitor. Synonyms: 2-Propyn-1-ol, 3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-7-(3-aminopropoxy)-1-ethyl-1H-imidazo[4,5-c]pyridin-4-yl]-. Grades: >98%. CAS No. 842148-40-7. Molecular formula: C16H19N7O3. Mole weight: 357.37.
AKT Kinase Inhibitor
AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 842148-40-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg. Product ID: HY-10249A.
AKT Kinase Inhibitor hydrochloride
AKT Kinase Inhibitor hydrochloride is an Akt kinase inhibitor with anti-tumor activity [1]. AKT Kinase Inhibitor (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 3026697-00-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-10249D.
Alk 5 Inhibitor II
Alk 5 Inhibitor II. Group: Biochemicals. Alternative Names: 2-[3-(6-Methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine; E 616452; RepSox; SJN 2511. Grades: Highly Purified. CAS No. 446859-33-2. Pack Sizes: 10mg. Molecular Formula: C17H13N5, Molecular Weight: 287.32. US Biological Life Sciences.
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ALK5 Inhibitor II hydrochloride
ALK5 inhibitor II was identified as a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5 (ALK5 autophosphorylation, IC50s = 4 nM, TGF-β cellular assay, IC50s = 18 nM, ALK5 binding in HepG2 cells, IC50s = 23 nM). This compound has been used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2 via inhibition of the TGF-β signaling pathway and induction of Nanog transcription. This product is a hydrochloride form. Synonyms: E 616452; RepSox; SJN 2511. Grades: ≥98%. CAS No. 446859-33-2. Molecular formula: C17H13N5·HCl. Mole weight: 323.8.
ALK inhibitor 1
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase. Synonyms: Benzenesulfonamide, 2-[[5-bromo-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-. Grades: >98%. CAS No. 761436-81-1. Molecular formula: C23H28BrN7O3S. Mole weight: 562.48.
ALK inhibitor 2
ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase. Synonyms: Benzenesulfonamide, 2-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-. Grades: >98%. CAS No. 761438-38-4. Molecular formula: C23H28ClN7O3S. Mole weight: 518.03.
A glutamine transport inhibitor selective for Na+-dependent amino acid transport system A. Used in studying the functional roles of neurotransmissions mediated by amino acids. Group: Biochemicals. Grades: Highly Purified. CAS No. 2566-34-9. Pack Sizes: 250mg. US Biological Life Sciences.
PRMT1,3,4 & 6 Inhibitor. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
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Aminopeptidase N Inhibitor
Membrane alanyl aminopeptidase is also known as alanyl aminopeptidase (AAP) or aminopeptidase N (AP-N), which is an enzyme that in humans is encoded by the ANPEP gene. Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM. Human aminopeptidase N is a receptor for one strain of human coronavirus that is an important cause of upper respiratory tract infections. Defects in this gene appear to be a cause of various types of leukemia or lymphoma. Synonyms: AP-N Inhibitor. Grades: ≥95%. CAS No. 596108-59-7. Molecular formula: C17H10N2O8. Mole weight: 370.27.
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)
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.
A cell-permeable benzimidazole that, in addition to its inhibitory potency against luciferase activity (IC50 <10nM), also activates AMPK signaling by increasing cellular ADP/ATP ratio via mitochondria respiration upcoupling, effectively activating AMPK & PGC-1alpha in muscle, but not liver, cell types both in cultures (5-20uM in rat L6 myotubes) in vitro and in db/db mice (15mg/kg/day via p.o.) in vivo. Reported to improve glucose and insulin tolerance of db/db mice without any apparent effects on body weight or food intake. Group: Biochemicals. Grades: Highly Purified. CAS No. 4529-96-8. Pack Sizes: 25mg. Molecular Formula: C??H??N?. US Biological Life Sciences.
An acetyl-L-arginine analog of TAME that serves as a negative control. TAME is an ubiquitin ligase inhibitor that specifically blocks Anaphase-Promoting Complex (APC) activation. Group: Biochemicals. Grades: Highly Purified. CAS No. 1784-05-0. Pack Sizes: 50mg. Molecular Formula: C?H??N?O? · HCl, Molecular Weight: 266.7. US Biological Life Sciences.
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Anaphase-Promoting Complex Inhibitor, TAME (TAME Hydrochloride)
TAME is a potent ubiquitin ligase inhibitor that specifically blocks Anaphase-Promoting Complex (APC) activation by directly binding to APC and disrupts the IR-tail-dependent interactions between APC and its activator proteins Cdc20 or Cdh1. It stabilizes APC substrates and is shown to inhibit cyclin proteolysis in mitotic Xenopus egg extract with an IC50=12uM. Group: Biochemicals. Grades: Highly Purified. CAS No. 1784-03-8. Pack Sizes: 50mg. Molecular Formula: C??H??N?O?S · HCl, Molecular Weight: 378.87. US Biological Life Sciences.
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APE1 Inhibitor III
APE1 Inhibitor III is a selective and competitive inhibitor of apurinic/apyrimidinic (AP) endonuclease 1 (APE1) with 2.0 micromolar activity against the purified APE1 enzyme. Synonyms: N-[3-(1,3-Benzothiazol-2-yl)-6-isopropyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]acetamide. Grades: 99%. CAS No. 524708-03-0. Molecular formula: C19H21N3OS2. Mole weight: 371.52.
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.
Cyclopeptide inhibitor of histone deactylases (HDACs). Inhibits HeLa cell proliferation (IC50=50-. Group: Biochemicals. Alternative Names: Cyclo- N-O-methyl-L-tryptophanyl-Lisoleucinyl- Dpipecolinyl- L-2-amino-8-oxodecanoyl. Grades: Highly Purified. CAS No. 183506-66-3. Pack Sizes: 1mg, 5mg. US Biological Life Sciences.
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Apoptosis inhibitor
Apoptosis inhibitor. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Apoptosis Inhibitor;2,2-Methylenebis-(1,3-cyclohexanedione). Product Category: Heterocyclic Organic Compound. Appearance: Off-white solid. CAS No. 54135-60-3. Molecular formula: C13H16O4. Mole weight: 236.2637. Purity: 0.96. IUPACName: 2-[(2,6-dioxocyclohexyl)methyl]cyclohexane-1,3-dione. Canonical SMILES: C1CC(=O)C(C(=O)C1)CC2C(=O)CCCC2=O. Density: 1.227 g/cm³. ECNumber: 258-989-1. Product ID: ACM54135603. Alfa Chemistry ISO 9001:2015 Certified. Categories: 2,2'-METHYLENEBIS(1,3-CYCLOHEXANEDIONE), Apoptosis inhibitor of macrophage.
Aprotinin, Bovine (Pancreatic trypsin inhibitor)
Aprotinin is a competitive serine protease inhibitor that inhibits trypsin, chymotrypsin, kallikrein and plasmin. Aprotinin forms stable complexes with and blocks the active sites of enzymes. Binding is reversible with most aprotinin-protease complexes, dissociating at pH >10 or <3. Effective concentration is equimolar with protease. Group: Biochemicals. Alternative Names: Antikrein; Antilysin; Antilysine; Aprostat; Aprotinin; BPTI; BPTI Trypsin Inhibitor; Basic Pancreatic Trypsin Inhibitor; Bayer A 128; Bovine Basic Pancreatic Trypsin Inhibitor; Bovine Pancreatic Trypsin Inhibitor; Bovine Trypsin Inhibitor; Fosten; Kallikrein-trypsin Inactivator; Kiker 52G; Kir Richter; Kunitz Pancreatic Trypsin Inhibitor; Kunitz Protease Inhibitor; Kunitz Trypsin Inhibitor; Kunitz-type Inhibitor; Kunitz-type Proteinase Inhibitor; Kunitz-type Trypsin Inhibitor; Onquinin; Pancreatic Basic Trypsin Inhibitor; Pancreatic Trypsin Inhibitor; Pancreatic Trypsin Inhibitor (Kunitz); Protease Inhibitor, Kunitz Type; RP 9921; Repulson; Trasuylol; Trasylol; Trazinin; Triazinin; Trypsin Inhibitor, Trasylol; Trypsin-kallikrein Inhibitor (Kunitz); Zymofren. Grades: Highly Purified. CAS No. 9087-70-1. Pack Sizes: 100mg, 250mg, 500mg, 1g. Molecular Formula: C???H???N??O??S?, Molecular Weight: 6511.45. US Biological Life Sciences.
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ARE Activator, BTZO-1 (Macrophage Migration Inhibitory Factor Antagonist II, 2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, MIF Antagonist II)
A cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (=68.6nM and 157nM toward human and rat MIF, respectively, at pH 7.3) via the N-terminal proline in a pH-dependent manner, limiting its inhibitory capability against MIF tautomerase activity (13% inhibition at pH 6.0; [BTZO-1] = 30uM) due to reduced MIF binding at acidic pH. Shown to protect primary rat cardiomyocytes (330nM) from apoptotic death upon serum deprivation or DOX (200nM) treatment via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription in a MIF-dependent manner. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H?N?OS, Molecular Weight: 240.3. US Biological Life Sciences.
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Arginase inhibitor 1
Arginase inhibitor 1 is active in a recombinant cellular assay overexpressing humanarginase I (CHO cells). It is 28% orally bioavailable and significantly reduces the infarct size in a rat model of myocardial ischemia/reperfusion injury. Synonyms: Arginase inhibitor 1. Grades: >98%. CAS No. 1345808-25-4. Molecular formula: C13H27BN2O4. Mole weight: 286.18.
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
ATP synthase inhibitor 1
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F 1 /F O -ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1023043-30-2. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112715.
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.
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ATR Inhibitor IV (VE821, 3-amino-6- (4- (methylsulfonyl) phenyl) -N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV)
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
ATR Kinase Inhibitor II (3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide)
A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12nM; Ki=6nM) with excellent selectivity over ATM, DNA-PK (IC50 > 8uM) and in a 50-kinase panel (% inhibition at 2uM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKK-alpha and FGFR3, respectively). Shown to block pH2AX-Ser139 (IC50 = 420nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin cytotoxicity against tumor cells over normal cells by ~7-fold at 620nM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences.
Worldwide
Aurora A Inhibitor I
Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B. Synonyms: TC-S 7010; TC S 7010; TCS7010. Grades: >98%. CAS No. 1158838-45-9. Molecular formula: C31H31ClFN7O2. Mole weight: 588.07.
Aurora A inhibitor II
Aurora A inhibitor II is a potent and selective inhibitor of Aurora A kinase (AurA; IC50 = 4.3 nM). Synonyms: 4-[[2-[[4-[2-(4-acetyl-1-piperazinyl)-2-oxoethyl]phenyl]amino]-5-fluoro-4-pyrimidinyl]amino]-N-(2-chlorophenyl)-Benzamide. Grades: 99%. CAS No. 1158838-43-7. Molecular formula: C31H29ClFN7O3. Mole weight: 602.06.
Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC 50 s of 310 nM and 240 nM for Aurora A and Aurora B , respectively [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 331770-21-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112355.
Aurora Kinase Inhibitor II
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A with IC50 of 0.39 μM. This compound has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. This compound has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. Synonyms: 4-(4?-Benzamidoanilino)-6,7-dimethoxyquinazoline. Grades: ≥98%. CAS No. 331770-21-9. Molecular formula: C23H20N4O3. Mole weight: 400.4.
Aurora Kinase Inhibitor III
Aurora kinase inhibitor III is a potent ATP-competitive aurora related kinase inhibitor with IC50 of 42 nM. Aurora kinase inhibitor III is a cell-permeable, 2,4-dianilinopyrimidine compound which has been used to study a variety of tumor types. It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). Aurora kinase protein levels are elevated in c-myc-driven B-cell lymphomas in both mice and humans. Study of the inhibition of Aurora kinase proteins could lead to potential treatments for malignancies. Synonyms: Aurora Kinase Inhibitor III; AKI-7169; AKI 7169; AKI7169. Grades: ≥98%. CAS No. 879127-16-9. Molecular formula: C21H18F3N5O. Mole weight: 413.4.
A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50=110 and 130nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50=0.88, 1.03 and 1.79uM for Lck, Src and MEK1, respectively, and IC50>10uM for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20uM, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 331771-20-1. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
Autocamtide-2-related inhibitory peptide
Autocamtide-2-related inhibitory peptide. Group: Biochemicals. Grades: Purified. CAS No. 167114-91-2. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
Autocamtide-2-Related Inhibitory Peptide
Autocamtide-2-related inhibitory peptide is a highly selective, specific and potent inhibitor of calmodulin-dependent protein kinase II (CaM kinase II) with I50 value of 40 nM. It is selective over PKC, PKA and CaM kinase IV. Synonyms: AIP; [Ala9]-Autocamtide 2. Grades: ≥97% by HPLC. CAS No. 167114-91-2. Molecular formula: C64H116N22O19. Mole weight: 1497.74.
Autocamtide-2-related inhibitory peptide, myristoylated is a CaM kinase II inhibitor. It is an enhanced cell-permeable derivative of autocamtide-2-related inhibitory peptide. It blocks reinstatement of morphine-seeking behavior in vivo by pretreatment. Synonyms: AIP Myristoylated; Myr-AIP. Grades: >98%. CAS No. 201422-04-0. Molecular formula: C78H142N22O20. Mole weight: 1708.12.
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