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MAPKinaseKinase 3,6 (MKK3,6) Control Cell Extracts
MAPKinaseKinase 3,6 (MKK3,6) Control Cell Extracts. Group: Biologicals. Grades: Lysate. Pack Sizes: 10Blots. US Biological Life Sciences.
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MAPKinaseKinase 3,6 (MKK3,6) Nonphosphorylated Control Cell Extract
Nonphosphorylated Control Cell Extract for M2363-15A. Total cell extracts from NIH/3T3 cells, prepared without treatment, serve as a negative control. Group: Molecular Biology. Pack Sizes: 200ul. US Biological Life Sciences.
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MAPKinaseKinase 3,6 (MKK3,6) Phosphorylated Control Cell Extract
MAPKinaseKinase 3,6 (MKK3,6) Phosphorylated Control Cell Extract. Group: Molecular Biology. Pack Sizes: 200ul. US Biological Life Sciences.
Nonphosphorylated Control Cell Extract for M2363-15A. Total cell extracts from NIH/3T3 cells, prepared without treatment, serve as a negative control. Group: Molecular Biology. Pack Sizes: 80ul. US Biological Life Sciences.
Phosphorylated Control Cell Extract for M2363-15A. Total cell extracts from NIH/3T3 cells, prepared with UV light treatment, serve as a positive control. Group: Molecular Biology. Pack Sizes: 80ul. US Biological Life Sciences.
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MAPKinase p38, Control Cell Extracts (Mitogen Activated Protein Kinase p38, MAPK p38)
P38 MAPkinase (MAPK), also called RK (3) or CSBP (2), is the mammalian homologue of the yeast HOG kinase and participates in a signaling cascade controlling cellular responses to cytokines and stress (1-4). Four isoforms of p38 MAPkinase, alpha, beta, gamma and delta, have been identified so far. Like the SAPK/JNK pathway, p38 MAPkinase is activated by a variety of cellular stresses including osmotic shock, inflammatory cytokines, lipopolysaccharides (LPS), UV light and growth factors (1-5). MKK3 and SEK activate p38 MAPkinase by phosphorylation at threonine 180 and tyrosine 182. Activated p38 MAPkinase has been shown to phosphorylate and activate MAPKAP kinase 2 (3) and to phosphorylate the transcription factors ATF-2 (5), Max (6) and MEF2 (5-8). Nonphosphorylated p38 MAPKinase Control Cell. Group: Biologicals. Alternative Names: EC=2.7.11.24. Grades: Lysate. Pack Sizes: 10Blots. US Biological Life Sciences.
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MAPK/MAK/MRK overlapping kinase (11-20)
MAPK/MAK/MRK overlapping kinase (11-20) is a 10-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
MAPK/MAK/MRK overlapping kinase (32-40)
MAPK/MAK/MRK overlapping kinase (32-40) is a 9-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
MAPK/MAK/MRK overlapping kinase (352-360)
MAPK/MAK/MRK overlapping kinase (352-360) is a 9-aa peptide. MAPK/MAK/MRK overlapping kinase is able to phosphorylate several exogenous substrates and to undergo autophosphorylation.
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.
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p38 MAPKinase Inhibitor IV
p38 MAPKinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC 50 s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1638-41-1. Pack Sizes: 5 mg. Product ID: HY-112401.
p38 MAPKinase Inhibitor XI (4-(2,4-Difluorophenyl)-8-(2-methylphenyl)-1,7-naphthyridine-7-oxide, 4-(2,4-Difluorophenyl)-8-o-tolyl-1,7-naphthyridine-7-oxide)
A cell-permeable naphthyridine N-oxide compound that acts as a potent, reversible p38alpha MAPkinase inhibitor (IC50 = 68nM) and exhibits excellent selectivity among 54-kinases. It acts on the ATP-binding site plus an adjacent hydrophobic pocket. Exhibits desirable ADME (Absorption, Distribution, Metabolism, and Excretion) profile with good microsomal stability, low toxicity, and low reactivity towards cytochrome P450 isozymes. Shown to inhibit lipopolysaccharide-induced TNF-alpha production in a dose-dependent manner (ED50 of 0.5mg/kg). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
A cell-permeable phenylamino-dibenzosuberone-diol with a rigid molecular structure specifically designed to target hydrophobic region I in p38alpha & p38beta, but not in other kinases with bulky entrance-blocking gatekeeper residues. Shown to selectively inhibit p38alpha (IC50 = 5nM; [ATP] = 100uM) and p38beta (97% inhibition at 1uM), while exhibiting little affinity toward 400 other kinase constructs, including p38delta, p38upsilon, Erk1/2/3/4/5/8, JNK1/2/3, and MEK1/2/3/4/6. Shown to prevent cellular HSP27 Ser82 phosphorylation upon p38 activation by Anisomycin in HeLa (IC50 = 25nM) or by TNF-alpha in THP-1 cultures. Unlike the ATP-binding site-targeting BIRB 796 and SB 203580, Skepinone-L does not inhibit JNK-mediated c-Jun or ERK-dependent CREB phosphorylation in THP-1 cultures. Oral administration to D-Gal-sensitized mice is reported to greatly reduce plasma TNF-alpha production upon LPS challenge (by 77%; 3mg/kg p.o.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
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1- (Chloromethyl) naphthalene
1- (Chloromethyl) naphthalene is used in the identification of Novel p38α MAPKinase Inhibitors. It is also used in the Identification of 1,5-Naphthyridine derivatives as a novel series of potent and selective TGF- β type I receptor inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 86-52-2. Pack Sizes: 1g, 5g. Molecular Formula: C11H9Cl. US Biological Life Sciences.
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1- methyl cyclohexanecarboxylic Acid
1- methyl cyclohexanecarboxylic Acid is used in the synthesis of p38 mapkinase. Group: Biochemicals. Alternative Names: 1-Methyl-1-cyclohexanecarboxylic Acid; 1- methyl cyclohexanecarboxylic Acid; 1- methyl cyclohexylcarboxylic Acid. Grades: Highly Purified. CAS No. 1123-25-7. Pack Sizes: 5g. US Biological Life Sciences.
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1- methyl cyclohexanecarboxylic Acid-d10
Isotope labelled 1- methyl cyclohexanecarboxylic Acid is used in the synthesis of p38 mapkinase. Group: Biochemicals. Alternative Names: 1-Methyl-1-cyclohexanecarboxylic Acid-d10; 1- methyl cyclohexanecarboxylic Acid-d10; 1- methyl cyclohexylcarboxylic Acid-d10. Grades: Highly Purified. Pack Sizes: 1mg. US Biological Life Sciences.
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20-Hydroxy-(5Z,8Z,11Z,14Z)-eicosatetraenoic acid
20-Hydroxy-(5Z,8Z,11Z,14Z)-eicosatetraenoic acid is a potent vasoconstrictor produced in vascular smooth muscle cells. Its EC50 value is < 10 nM. It is a cytochrome P450 metabolite. It induces diuresis by inhibiting Na+-K+-ATPase in proximal tubules and Na+/K+/Cl+ cotransporter in the thick ascending limb of Henle's loop in kidney. It is involved in the regulation of sodium, potassium, and chloride transport in the renal tubules. It is a vasoconstrictor that mediates pressure-induced autoregulatory vasoconstriction in rat cerebral microvessels. It is excreted mainly as the glucuronide conjugate. It can be further metabolized by cyclooxygenase to 20-hydroxy PGG2 and 20-hydroxy PGH2. It regulates blood pressure in a complex way. It sensitizes smooth muscle cells to the constrictor stimuli and promotes the proliferation of endothelial cells. It has the ability to induce proinflammatory changes. It blocked the 70 pS K+ channel localized in the apical membrane in TALH cells. It was found to be a potent vasoconstrictor through activating the kinase pathways that contribute to the vascular tone regulation including MAPK, PKC, rho kinase and src-type tyrosine kinase. It may similarly regulate blood pressure and contribute to the development of stroke and heart attacks. Synonyms: 20-Hydroxyeicosatetraeonic acid; 20 Hydroxyeicosatetraeonic acid; 20Hydroxyeicosatetraeonic acid; 20HETE; 20 HETE; 20-HETE;(5Z,8Z,11Z,14Z)-20-hydroxyicosa-5,8,11,14-tetraenoic acid;20-Hydroxyeicosatetraenoic acid;20-hydroxy-5,8,11,14-eicosatetraenoic acid. Grades: >98%. CAS No. 79551-86-3. Molecular formula: C20H32O3. Mole weight: 320.47.
2-(1-Hexyn-1-yl)benzoic Acid
2-(1-Hexyn-1-yl)benzoic Acid is an intermediate in synthesizing Apigenin 5-O- β-D-Glucuronide (A426510), a metabolite of Apigenin (A726500), Induces the reversion of transformed phenotypes of v-H-ras-transformed NIH 3T3 cells at low concentration (12.5 uM) by inhibiting MAPkinase activity. Also inhibits the proliferation of malignant tumor cells by G2/M arrest and induces morphological differentiation. Apigenin has also been reported to enhance the gap junction intracellular communication in liver cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 120870-47-5. Pack Sizes: 250mg, 500mg. Molecular Formula: C13H14O2. US Biological Life Sciences.
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2,3-Dihydro-1H-indene-5-carbonyl Chloride
2,3-Dihydro-1H-indene-5-carbonyl Chloride is a compound involved in the discovery of a class of potent N-pyrimidyl amide based p38a MAPkinase inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 15497-40-2. Pack Sizes: 100mg, 250mg. Molecular Formula: C10H9ClO, Molecular Weight: 180.63. US Biological Life Sciences.
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2-(3-Phenyl-4,5-dihydroisoxazol-5-yl)acetic Acid
2-(3-Phenyl-4,5-dihydroisoxazol-5-yl)acetic Acid reduces the secretion of IL-1 β, TNF-α and IL-10 from purified murine macrophages but not of T cells; and reduces the activation of NF-κB and p38 MAPkinase pathways along with up-regulation of ERK pathways. 2-(3-Phenyl-4,5-dihydroisoxazol-5-yl)acetic Acid inhibits proliferation of enterobacterial antigen-reactive CD4+CD25- T cells in vitro. Group: Biochemicals. Grades: Highly Purified. CAS No. 6501-72-0. Pack Sizes: 5mg, 10mg. Molecular Formula: C11H11NO3, Molecular Weight: 205.21. US Biological Life Sciences.
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(2,4-Difluorophenoxy)acetic Acid Methyl Ester
(2,4-Difluorophenoxy)acetic Acid Methyl Ester is an intermediate in the synthesis of Pamapimod (P167500), a selective inhibitor of the α-isoform of p38 MAPkinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 449811-63-6. Pack Sizes: 100mg, 250mg. Molecular Formula: C9H8F2O3. US Biological Life Sciences.
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2'-O-Me-cGMP
2'-O-Me-cGMP is a polar analogue of cGMP that activate neither protein kinase G nor Epac. It exhibits an inactive effect in patch clamp applications and can be used for receptor mapping studies. Synonyms: 2'- O- Methylguanosine- 3', 5'- cyclic monophosphate, sodium salt. Grades: ≥ 98% by HPLC. CAS No. 949909-73-3. Molecular formula: C11H13N5O7P · Na. Mole weight: 381.2.
3- (2, 4-Dimethoxyphenyl) propionic Acid
3- (2, 4-Dimethoxyphenyl) propionic Acid acts as a synthetic reagent in the preparation of acyl aminopyridinyl imidazoles as p38 MAPkinase inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 22174-29-4. Pack Sizes: 250mg, 1g. Molecular Formula: C11H14O4, Molecular Weight: 210.23. US Biological Life Sciences.
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3-Amino-1,5-pentanediol
3-Amino-1,5-pentanediol is an substituent in the synthesis of Pamapimod (P167500), a selective inhibitor of the α-isoform of p38 MAPkinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 1117-23-3. Pack Sizes: 10mg, 50mg. Molecular Formula: C5H13NO2. US Biological Life Sciences.
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3-[(Phenylmethyl)amino]-1,5-pentanediol
3-[(Phenylmethyl)amino]-1,5-pentanediol is an protected substituent in the synthesis of Pamapimod (P167500), a selective inhibitor of the α-isoform of p38 MAPkinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 1034082-96-6. Pack Sizes: 25mg, 100mg. Molecular Formula: C12H19NO2. US Biological Life Sciences.
3-[ (Phenylmethyl) amino]pentanedioic Acid Dimethyl Ester 3-[ (Phenylmethyl) amino]pentanedioic Acid Dimethyl Ester is an protected substituent in the synthesis of Pamapimod (P167500), a selective inhibitor of the α-isoform of p38 MAPkinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 109270-76-0. Pack Sizes: 50mg, 250mg. Molecular Formula: C14H19NO4. US Biological Life Sciences.
Potential inhibitor of glucagon receptors, also used in the synthesis of p38 MAPkinase inhibitors. Group: Biochemicals. Alternative Names: 4-[5-(4-Fluorophenyl)-2-[4-(methylthio)phenyl]-1H-imidazol-4-yl]pyridine. Grades: Highly Purified. CAS No. 152121-44-3. Pack Sizes: 25mg. US Biological Life Sciences.
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(+)-[6]-Gingerol
(+)-[6]-Gingerol is a bioactive compound found in ginger (Zingiber officinale) with antioxidant activity, which functions as an anti-inflammatory and antitumor agent. (+)-[6]-Gingerol down regulates proinflammatory cytokine release by macrophages. (+)-[6]-Gingerol has been shown to inhibit COX-2 expression by blocking the activation of p38 MAPkinase and NF-κB in phorbol ester-stimulated mouse skin. Group: Biochemicals. Alternative Names: (5S)-5-Hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-decanone; (S)-(+)-5-Hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-decanone; (+)-5-Hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-decanone; (5S)-[6]-Gingerol; (S)-(+)-[6]Gingerol; (S)-[6]Gingerol; [6]-Gingerol. Grades: Highly Purified. CAS No. 23513-14-6. Pack Sizes: 10mg. US Biological Life Sciences.
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8-TEMPO-aminoadenosine Cyclic 3',5'-Monophosphate
8-TEMPO-aminoadenosine Cyclic 3',5'-Monophosphate, a spin-labeled cyclic nucleotide used for the mapping of the cAMP site of protein kinase I from rabbit skeletal muscle. Synonyms: 4-[[6-Amino-9-(3,5-O-phosphinico-β-D-ribofuranosyl)-9H-purin-8-yl]amino]-2,2,6,6-tetramethyl-1-piperidinyloxy; 4H-Furo[3,2-d]-1,3,2-dioxaphosphorin, 1-Piperidinyloxy Deriv. CAS No. 54606-91-6. Molecular formula: C19H29N7O7P. Mole weight: 498.45.
A431+ EGF (5min) Lysate
A431 cells express approximately 10e6 epidermal growth factor (EGF) receptors at the cell surface. Upon stimulation with EGF, A431 cells exhibit a dramatic increase in phosphorylation of EGF receptors followed by activation of major cell signaling pathways, such as PKB/Akt and MAPkinase pathways. Downstream of these cell signaling pathways, a variety of cytoskeletal, cytoplasmic, and nuclear proteins become phosphorylated at different time points after EGF stimulation. Group: Biologicals. Grades: Lysate. Pack Sizes: 100ug. US Biological Life Sciences.
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Acumapimod
Acumapimod (BCT197) is an orally active p38 MAPkinase inhibitor, with an IC 50 of less than 1 μM for p38&alpha. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BCT197. CAS No. 836683-15-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-16715.
AG 825
AG 825, a selective ErbB2 (Neu) inhibitor, could probably show activities in triggerring p38 MAPkinase-dependent apoptosis at some extent. Synonyms: AG 825; AG825; AG-825; (E)-3-[3-[2-Benzothiazolythio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide. Grades: ≥95% by HPLC. CAS No. 149092-50-2. Molecular formula: C19H15N3O3S2. Mole weight: 397.47.
Akt/SKG Substrate Peptide
Akt/SKG Substrate Peptide is a synthetic peptide and used as a substrate for Akt/PKB. It could not be phosphorylated by MAPkinase or p70 S6 kinase activated protein kinase-1. Synonyms: N5-(Diaminomethylene)-L-ornithyl-L-prolyl-N5-(diaminomethylene)-L-ornithyl-L-alanyl-L-alanyl-L-threonyl-L-phenylalanine. CAS No. 276680-69-4. Molecular formula: C36H59N13O9. Mole weight: 817.95.
Aminopurvalanol A
Aminopurvalanol A is a selective, cell-permeable, reversible and ATP-competitive cyclin-dependent kinase (CDK) inhibitor. It is a 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties. It induces cell differentiation by preferentially targeting the G2/M-phase and acts intracellularly by inhibiting both Cdks and MAPKs. It potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 with IC50s values of 33, 33, 28, and 20 nM, respectively. It also inhibits growth of ovarian leukemic (SR), (IGROV1), colonic (KM12) and lung (NCI-H522) cells in antiproliferative assays in vitro. Synonyms: (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol; NG-97; NG97; NG 97; Aminopurvalanol A; Aminopurvalanol-A. Grades: ≥98% by HPLC. CAS No. 220792-57-4. Molecular formula: C19H26ClN7O. Mole weight: 403.91.
Ammocidin
It is produced by the strain of Saccharothrix sp. AJ 9571. It can reduce the phosphorylation level of mitogen-activated protein kinase (MAPK)S6K. It induces apoptosis in Ras Ba/F3-V12 cells with an IC50 of 66 ng/mL, but not in IL-3 Ba/F3-V12 cells with 100 μg/mL. Synonyms: Ammocidin A. Molecular formula: C59H96O21. Mole weight: 1141.38.
Anisomycin (Flagecidin, Antibiotic SA 3097C1, Antibiotic PA 106, Anhydroscopin A, NSC)
Anisomycin is a phenyl methyl enepyrrolidine first isolated from Streptomyces griseolus in 1954 as an antiprotozoan with antifungal activity. Anisomycin acts as an inhibitor of protein synthesis by binding to the 60S ribosomal subunit. Interestingly, anisomycin has found use for the induction of amnesia in animal models. More recently, anisomycin has been demonstrated to induce apoptosis, to be a selective signalling agonist, to activate mitogen-activated protein (MAP) kinases and to be immunomodulatory via its action on T cells. Group: Biochemicals. Alternative Names: ((2R,3S,4S)-2-(4-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate, 2-[(4-Methoxyphenyl)methyl]-3,4-pyrrolidinediol 3-acetate. Grades: Highly Purified. CAS No. 22862-76-6. Pack Sizes: 25mg, 100mg, 250mg. US Biological Life Sciences.
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anthrax lethal factor endopeptidase
From the bacterium Bacilus anthracis that causes anthrax. One of three proteins that are collectively termed anthrax toxin. Cleaves several MAPkinasekinases near their N-termini, preventing them from phosphorylating the downstream mitogen-activated protein kinases. In peptidase family M34. Group: Enzymes. Synonyms: lethal toxin. Enzyme Commission Number: EC 3.4.24.83. CAS No. 477950-41-7. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-4367; anthrax lethal factor endopeptidase; EC 3.4.24.83; 477950-41-7; lethal toxin. Cat No: EXWM-4367.
Antibiotic LL Z1640-4 (Zeaenol)
Antibiotic LL Z1640-4 is a cis-enol resorcylic acid lactone first reported in 1978 exhibiting both antiviral and antiprotozoan activity. More recently, antibiotic LL Z1640-2 containing the essential cis-enone system that selectively inhibits TAK 1 has gained literature focus. With its inactive cis-enol, Antibiotic LL Z1640-4 is an ideal negative control to help dissect the selectivity of the MAPkinases. Group: Biochemicals. Alternative Names: Zeaenol. Grades: Highly Purified. CAS No. 66018-41-5. Pack Sizes: 1mg. US Biological Life Sciences.
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Apigenin (4',5,7-Trihydroxyflavone)
Induces the reversion of transformed phenotypes of v-H-ras-transformed NIH 3T3 cells at low concentration (12.5 uM) by inhibiting MAPkinase activity. Also inhibits the proliferation of malignan. Group: Biochemicals. Alternative Names: 4',5,7-Trihydroxyflavone. Grades: Highly Purified. Pack Sizes: 100mg. US Biological Life Sciences.
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Apigenin-d5 7-Glucuronide
Apigenin-d5 7-Glucuronide is labelled Apigenin 7-Glucuronide (A726505), a metabolite of Apigenin, which induces the reversion of transformed phenotypes of v-H-ras-transformed NIH 3T3 cells at low concentration (12.5 uM) by inhibiting MAPkinase activity. Also inhibits the proliferation of malignant tumor cells by G2/M arrest and induces morphological differentiation. Apigenin has also been reported to enhance the gap junction intracellular communication in liver cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 10mg. Molecular Formula: C21H13D5O11, Molecular Weight: 451.39. US Biological Life Sciences.
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ARQ 736 disodium salt
This active molecular is a Proto oncogene protein b raf and Vascular endothelial growth factor A inhibitor originated by ArQule. ARQ 736 is effective in killing cancer cell lines that harboring at least one mutated b raf allele. The b raf protein is really a very important signaling molecule in the MAPK (mitogen activated protein kinase) signaling pathway and it relates to pathogenesis of variety kinds of cancer. In Mar 2014, Phase-I for Solid tumours (late-stage disease) was discontinued in USA. Uses: Solid tumours. Synonyms: ARQ 736 disodium salt; ARQ736 disodium salt; ARQ-736 disodium salt; sodium (R)-(3-(5-(2-((1-((1-methyl-1H-pyrazol-3-yl)sulfonyl)piperidin-3-yl)amino)pyrimidin-4-yl)imidazo[2,1-b]oxazol-6-yl)phenoxy)methyl phosphate;1228237-47-5 free acid. Grades: 98%. CAS No. 1228237-57-7. Molecular formula: C25H25N8Na2O8PS. Mole weight: 674.54.
AS1940477
AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg/kg (ED(50)=0.053 mg/kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this study demonstrated that AS1940477 is a novel and potent p38 MAPK inhibitor and may be useful as a promising anti-inflammatory agent for treating inflammatory disorders. Synonyms: AS1940477; AS-1940477; AS 1940477. CAS No. 928344-12-1. Molecular formula: C24H22FN5O2. Mole weight: 431.47.
Asiaticoside
Antibacterial. Human collagen I synthesis inducer. Anti-wrinkle activity. Shows wound healing activity. Enhances normal human skin cell migration, attachment and growth. Suppresses collagen expression and TGF-beta/Smad signaling by inducing Smad7 and inhibiting TGF-betaRI and TGF-betaRII. Anti-inflammatory. Anti-gastric ulcer. Mitogen-activated protein kinases (MAPKs), nuclear factor-kappaB (NF-kappaB), cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS; NOSII) expression, production of serum tumor necrosis factor (TNF-alpha) and interleukin-6 (IL-6) inhibitor. Apoptosis inducer in cancer cells. Enhances antitumor activity of vincristine in cancer cells. Might be useful in cancer chemotherapy. Anxiolytic. Antidepressant-like activity. Hepatoprotective effects. CYP2C19 and CYP3A4 inhibitor. Neuroprotective. Antileishmanial activity. cPLA2 and sPLA2 inhibitor. Group: Biochemicals. Alternative Names: Blastostimulina, Centelase, Emdecassol, Madecassol, Marticassol, FK1080, BRN 0078195, NSC 166062. Grades: Highly Purified. CAS No. 16830-15-2. Pack Sizes: 10mg, 50mg. Molecular Formula: C48H78O19. US Biological Life Sciences.
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Atorvastatin-d5 Lactone
Labeled Atorvastatin intermediate as inhibitor of MAPkinase and/or HMG-CoA reductase for the treatment of inflammation. Group: Biochemicals. Alternative Names: 5-(4-Fluorophenyl)-2-(1-methylethyl)-N-phenyl-(4-phenyl-d5)-1-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1H-pyrrole-3-carboxamide; Atorvastatin-d5 δ-Lactone. Grades: Highly Purified. CAS No. 1217749-86-4. Pack Sizes: 1mg. Molecular Formula: C??H??D?FN?O?, Molecular Weight: 545.66. US Biological Life Sciences.
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AZD-8330
AZD8330 is an orally active, selective MEK inhibitor with potential antineoplastic activity. AZD8330 specifically inhibits mitogen-activated protein kinasekinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. Synonyms: AZD8330; AZD-8330; AZD 8330; ARRY424704; ARRY 424704; ARRY-424704; ARRY704; ARRY-704; ARRY 704. Grades: 0.98. CAS No. 869357-68-6. Molecular formula: C16H17FIN3O4. Mole weight: 461.232.
Berberine chloride hydrate
The plant-based alkaloid berberine has potential therapeutic applications for breast cancer, although a better understanding of the genes and cellular pathways regulated by this compound is needed to define the mechanism of its action in cancer treatment. In this review, the molecular targets of berberine in various cancers, particularly breast cancer, are discussed. Berberine was shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells. Some signaling pathways affected by berberine, including the MAP (mitogen-activated protein) kinase and Wnt/β-catenin pathways, are critical for reducing cellular migration and sensitivity to various growth factors. Treatment with BBR(Berberine) in rats on the atherogenic diet reduced plasma total cholesterol and nonHDL cholesterol levels by 29%-33% and 31%-41%, respectively, with no significant differences being observed among the three doses. Berberine induced both apoptotic and autophagic death of HepG2 cells, which was associated with a significant activation of AMPK and an increased expression of the inactive form of acetyl-CoA carboxylase (ACC). Berberine did not show major effects on viability of HEK-293 embryonic kidney and HCT116 colon carcinoma cells and was not toxic in concentrations up to 20 μM. Berberine inhibited β-catenin transcriptional activity and attenuated anchorage-independent growth. As a result of berberine treatment, cellular levels of active β-catenin were reduced concomitant with an increase in the expression of E-cadherin. Synonyms: Natural Yellow 18. Grades: >98%. CAS No. 141433-60-5. Molecular formula: C20H18ClNO4. Mole weight: 371.81.
BIBU 1361 dihydrochloride
BIBU 1361 dihydrochloride is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM) with ~ 100-fold lower potency than ErbB2 (IC50 = 290 nM) and selectivity over a range of other related tyrosine kinases (IC50 > 10 μM). BIBU 1361 blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Synonyms: BIBU 1361 dihydrochloride; BIBU1361 dihydrochloride; BIBU-1361 dihydrochloride; N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride. Grades: ≥97% by HPLC. CAS No. 793726-84-8. Molecular formula: C22H27ClFN7.2HCl. Mole weight: 516.87.
Bisindolylmaleimide III
Bisindolylmaleimide III is a potent and selective inhibitor of PKC (protein kinase C) with structural similarity to the nonspecific PKC inhibitor staurosporine. It inhibits 93% of PKCα kinase activity and also inhibits many other protein kinases including, S6K1, MAPKAP-K1, RSK2 and MSK1. Synonyms: BIM III. Grades: ≥98%. CAS No. 137592-43-9. Molecular formula: C23H20N4O2. Mole weight: 384.4.
BMS582949
BMS582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 value of 13nM, which plays a crucial role in regulating the biosynthesis of many inflammatory cytokines including TNFα and IL-1&beta. It is used for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers Squibb and was in clinic phase 2 trials, but now it is terminated. Uses: Bms582949 is used for the treatment of rheumatoid arthritis. Synonyms: 4-[[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;BMS-582949;PS-540446; BMS 582949; PS 540446; BMS582949; PS540446. Grades: 98%. CAS No. 623152-17-0. Molecular formula: C22H26N6O2. Mole weight: 406.49.
BMS-582949 hydrochloride
BMS-582949 hydrochloride is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 of 13 nM. It displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases including serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. It does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 in vitro. It exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. It is currently under Phase II clinical trials for the treatment of inflammatory diseases. Uses: Bms-582949 hydrochloride is used for the treatment of inflammatory diseases. Synonyms: BMS 582949 hydrochloride; BMS582949 hydrochloride; BMS-582949 hydrochloride; 4-((5-((Cyclopropylamino)carbonyl)-2-methylphenyl)amino)-5-methyl-n-propylpyrrolo(2,1-f)(1,2,4)triazine-6-carboxamide. Grades: >98%. CAS No. 912806-16-7. Molecular formula: C22H27ClN6O2. Mole weight: 442.94.
BQ-123 Sodium Salt
Potent and selective endothelin receptor A (ETA) antagonist. Suppresses the ET-1-induced decrease of LPL activity. Shows protective effects in ischemic acute renal failure. Neuroprotective. Anti-hypertensive. Inhibits ET-1 receptor binding and blocks Ca2+ mobilization, cellular contraction and MAPkinase activation. Cardiovascular agent. Reduces myocardial infarct size and oxidant injury. Source:Synthetic. Group: Biochemicals. Grades: Highly Purified. CAS No. 136553-81-6. Pack Sizes: 1mg, 5mg. Molecular Formula: C31H42N6O7 Na. US Biological Life Sciences.
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Braftide
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC 50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells ( EC 50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence [1]. Uses: Scientific research. Group: Peptides. CAS No. 2411851-64-2. Pack Sizes: 5 mg; 10 mg. Product ID: HY-P10436.
Butein
Butein is a cAMP-specific PDE inhibitor with an IC 50 of 10.4 μM for PDE4 [1]. Butein is a specific protein tyrosine kinase inhibitor with IC 50 s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells [2]. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a [3]. Butein is a SIRT1 activator (STAC). Uses: Scientific research. Group: Natural products. Alternative Names: 2,3,4,4-tetrahydroxy Chalcone. CAS No. 487-52-5. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-16558.
A biologically active, cell permeable, but nonphysiologic ceramide analog. It inhibits cell proliferation and induces monocytic differentiation of HL-60 cells and induces apoptosis. It stimulates protein phosphatase 2A and activates MAPKinase2. Group: Biochemicals. Alternative Names: N-[(1S,2R,3E)-2-Hydroxy-1-(hydroxymethyl)-3-heptadecen-1-yl]acetamide; N-Acetyl-D-sphingosine; Acetyl Ceramide; N-Acetylsphingosine. Grades: Highly Purified. CAS No. 3102-57-6. Pack Sizes: 5mg, 10mg, 25mg, 50mg. Molecular Formula: C??H??NO?, Molecular Weight: 341.53. US Biological Life Sciences.
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C6 Ceramide-13C2,d2
A biologically active, cell permeable, but nonphysiologic ceramide analog. It stimulates protein phosphatase 2A at concentrations as low as 10 nM and activiates MAPkinase. It induces apoptosis and inhibits glycoproptein traffic by the secretory pathway. Group: Biochemicals. Alternative Names: N-Hexanoy-D-sphingosine-13C2,d2; N-Caproyl-D-sphingosine-13C2,d2; Caproyl Ceramide-13C2,d2. Grades: Highly Purified. Pack Sizes: 500ug. US Biological Life Sciences.
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CAY10561
The extracellular signal-regulated kinases (ERKs) or classical MAPkinases are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 with Ki of 2 nM. It is highly selective for ERK2 and inhibits proliferation of COLO 205 cells with IC50 of 0.54 μM. Synonyms: Pyrazolylpyrrole ERK Inhibitor; CAY 10561; CAY-10561. Grades: ≥98%. CAS No. 933786-58-4. Molecular formula: C22H17Cl2FN4O2. Mole weight: 459.3.
CAY10571
CAY10571 is a cell-permeable, reversible, and ATP-competitive sulfone analog of the p38 MAPkinase inhibitor. It is an analog of SB203580, which inhibits IL-1 production in the human monocytic cell line THP with an IC50 value of 0.20 μM and binds CSAID binding protein. Synonyms: CAY 10571; CAY-10571. Grades: ≥95%. CAS No. 152121-46-5. Molecular formula: C21H16FN3O2S. Mole weight: 393.4.
CBP501
CBP501 is a peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle. Check for active clinical trials or closed clinical trials using this agent. Synonyms: CBP-501; CBP 501; H-D-Bpa-D-Ser-D-Trp-D-Ser-D-Phe(F5)-D-Cha-D-Arg-D-Arg-D-Arg-D-Gln-D-Arg-D-Arg-OH. CAS No. 565434-85-7. Molecular formula: C86H122F5N29O17. Mole weight: 1929.06.
CC-90003
Extracellular-signal regulated kinases (ERKs) are a specific subtype of MAPK that have been extensively linked to regulation of synaptic plasticity and memory formation in many systems. CC-90003 is an irreversible and selective inhibitor of ERK1/2 with IC50s in the 10-20 nM range, which shows good kinase selectivity and antitumor activity in a 258-kinase biochemical assay. Synonyms: CC90003; CC 90003. Grades: ≥98%. CAS No. 1621999-82-3. Molecular formula: C22H21F3N6O2. Mole weight: 458.44.
Cercosporamide
Cercosporamide is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2) and JAK3. Cercosporamide effectively inhibits eIF4E phosphorylation as well as inibitiing inhibits Pkc1. Cercosporamide displays antiproliferative and proapoptotic activity in cancer cells in vitro. Group: Biochemicals. Alternative Names: (9aS) -8-Acetyl -9, 9a-di hydro-1, 3, 7-tri hydroxy-9a- methyl -9-oxo-4-dibenzofurancarboxamid e ; (S)-8-Acetyl -9, 9a-di hydro-1, 3, 7-tri hydroxy-9a- methyl -9-oxo-4-dibenzofurancarboxamid e ; (-)-Cercosporamide. Grades: Highly Purified. CAS No. 131436-22-1. Pack Sizes: 1mg. US Biological Life Sciences.
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Chelerythrine chloride
Cell permeable potent inhibitor of protein kinase C. Does not inhibit tyrosine protein kinases, cAMP-dependent protein kinase or calcium/calmodulin-dependent protein kinase. Antiplatelet, anti-inflammatory, antibacterial and antitumor compound. Apoptosis inducer in cancer cells in vitro and in vivo. Activates MAPK and JUNK signaling pathways. Affects translocation of PKC from cytosol to plasma membrane. Neurite outgrowth stimulator. Inhibits binding of BclXL to Bak (IC50 =1.5uM) or Bad proteins and stimulates apoptosis in several cancer cell lines. Blocks human P2X7 receptor. Induces cell cycle arrest in G1 phase. Specific cyclooxygenase-2 inhibitor. Group: Biochemicals. Alternative Names: NSC 36405, 1,2-Dimethoxy-N-methyl-[1,3]benzodioxolo[5,6-c]phenanthridinium chloride. Grades: Highly Purified. CAS No. 3895-92-9. Pack Sizes: 1mg, 5mg, 25mg. Molecular Formula: C21H18ClNO4. US Biological Life Sciences.
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Chidamide
Chidamide, also known as CS055 and HBI-8000, is an orally bioavailable benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Chidamide selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life. Synonyms: CS055; CS-055; CS 055; HBI-8000; HBI 8000; HBI8000; N-(2-amino-5-fluorophenyl)-4-[[[1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]-benzamide. CAS No. 743420-02-2. Molecular formula: C22H19FN4O2. Mole weight: 390.418.
CHMFL-BMX-078
CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor that exhibits an IC50 of 11 nM against BMX kinase and exhibits great selectivity over kinases such as BTK, JAK3, EGFR, and MAP2K7 that bore a structurally identical cysteine residue in BMX kinase. Uses: Protein kinase inhibitors. Synonyms: CHMFL-BMX-078; CHMFL-BMX 078;CHMFL BMX 078; CHMFLBMX078; 4- (methylamino) -2-[4-methyl-3- (prop-2-enoylamino) anilino]-N-[2-methyl-5-[ (3, 4, 5-trimethoxybenzoyl) amino]phenyl]pyrimidine-5-carboxamide; 2-((3-acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide. CAS No. 1808288-51-8. Molecular formula: C33H35N7O6. Mole weight: 625.67.
A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-a inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10uM, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10uM, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-a transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50=5-10uM), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08mg/g daily dose for 8 days without obvious toxicity, in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 1001478-90-5. Pack Sizes: 5mg. US Biological Life Sciences.
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c-Jun Control Cell Extracts
C-Jun is a component of the transcription factor AP-1 that binds and activates transcription at TRE/AP-1 elements. The transcriptional activity of c-Jun is regulated by phosphorylation at Ser63 and Ser73 (1,2). Extracellular signals including growth factors, transforming oncoproteins and UV irradiation stimulate phosphorylation of c-Jun at Ser63/73 and activate c-Jun dependent transcription. Mutation of Ser63/73 renders c-Jun nonresponsive to mitogenic and stress induced signaling pathways. The MAPkinase homologue, SAPK/JNK, binds to the N-terminal region of c-Jun and phosphorylates c-Jun at Ser63/73. In addition, the activity of SAPK/JNK is stimulated by the same signals that activate c-Jun (3,4). Nonphosphorylated c-Jun (Ser63) II Cell Extracts: Total cell extracts from NIH/3T3 cells, prepared without treatment, serve as a negative control. Group: Biologicals. Grades: Lysate. Pack Sizes: 10Blots. US Biological Life Sciences.
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CMPD-1
CMPD-1, also called MK2a Inhibitor, inhibits tubulin polymerisation. It inhibit p38α-mediated MK2a phosphorylation (apparent Ki = 330 nM). Synonyms: CMPD1; CMPD-1; CMPD 1; IN1225; IN-1225; IN 1225; 4-[4-(2-fluorophenyl)phenyl]-N-(4-hydroxyphenyl)butanamide; MK2a Inhibitor; MAPKAPK2a Inhibitor; CMPD1; CHEMBL235658; 41179-33-3; IN1225; 4-(2' -Fluorobiphenyl-4-yl)-N-(4-hydroxyphenyl)-butyramide; Mitogen-activated protein kinase-activated protein kinase 2a Inhibitor; MK2a Inhibitor_x000D_; SCHEMBL169905. CAS No. 41179-33-3. Molecular formula: C22H20FNO2. Mole weight: 349.4.
Cobimetinib racemate
Cobimetinib racemate is a selective inhibitor of MEK. It is also known as mitogen activated protein kinasekinase (MAPKK) and is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Synonyms: GDC-0973 racemate; XL-518; GDC 0973 racemate; XL 518; GDC0973 racemate; XL518. Grades: >98%. CAS No. 934662-91-6. Molecular formula: C21H21F3IN3O2. Mole weight: 531.31.
Cobimetinib (R-enantiomer)
Cobimetinib (R-enantiomer) is a selective inhibitor of MEK. It is also known as mitogen activated protein kinasekinase (MAPKK) and is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Synonyms: GDC-0973 R-enantiomer; XL-518 R-enantiomer; GDC0973 R-enantiomer; XL518 R-enantiomer; GDC 0973 R-enantiomer; XL 518 R-enantiomer. Grades: >98%. CAS No. 934660-94-3. Molecular formula: C21H21F3IN3O2. Mole weight: 531.31.
Coptisine sulfate
Coptisine sulfate is a natural compound that belongs to the group of plant alkaloids. It has been shown to have anti-inflammatory properties, significant cytotoxicity, and significant mitochondrial membrane potential in myeloma cells. Coptisine sulfate inhibits toll-like receptor 4 (TLR4), which is a protein present on the surface of immune cells. Coptisine sulfate has been shown to inhibit the production of cytokines such as tumor necrosis factor alpha (TNF-α) and IL-6 by these cells. Coptisine sulfate also inhibits the activation of nuclear factor kappa B (NFκB) and mitogen activated protein kinase (MAPK). This inhibition leads to reduced levels of proinflammatory cytokines and chemokines, such as IL-1β, IL-8, MCP1, and GRO&alpha. Group: Other alkaloids. CAS No. 1198398-71-8. Molecular formula: C38H28N2O12S. Mole weight: 736.7 g/mol. Canonical SMILES: C1C[N+]2=C (C=C3C=CC4=C (C3=C2)OCO4)C5=CC6=C (C=C51)OCO6. Catalog: ACM1198398718.
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