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Home > Biochemical Engineering > Inhibitors (Find 39 items)

Inhibitors

2-Cyano-3-hydroxy-N-(4-trifluoromethylphenyl)crotonamide

(108605-62-5)
The active metabolite of Leflunomide, a potent disease-modifying antirheumatic drug used in the treatment of rheumatoid arthritis.LEF-M interferes with dendritic cell function

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2-(Difluoromethyl)-1-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-1H-benzimidazole

(475110-96-4)
ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110β, -γ, and -δ, respectively). It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 μM. ZSTK474 is orally bioavailable and shows strong antitumor activity against human cancer xenografts in mice. The efficacy of ZSTK474 against certain cancer cells and tumors can be enhanced by combination therapy.

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2-[1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-1-(4-morpholinyl)ethanone

(2854-32-2)
BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively). IC50 Value: 435 nM(Ki CB2)Target:CB2 receptorin vitro: BML-190 increases the accumulation of cAMP, via forskolin-stimulated mechanism in HEK-293 cells. Alternate studies suggest that BML-190 reduces the toxicity of culture supernatants to SH-SY5Y human neutroblastoma cells. Various research suggests that BML-190 is an essential tool in studying the proliferation of

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2-Chloro-5-nitro-N-4-pyridinylbenzamide

(313516-66-4)
A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPAR with a Ki of 1 nM. Displays >800-fold greater selectivity for PPAR over PPARa and PPARd (Ki = 0.85and 1.8 ,

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2-Phenylethynesulfonamide

(64984-31-2)
A small molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation

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2-Chloro-5-nitrobenzanilide

(22978-25-2)
A cell-permeable, selective and irreversible PPAR antagonist (IC50 = 3.3 nM, 32 nM, and 2for PPAR, PPARa, and PPARd, respectively). Reported to covalently modify a cysteine residue in the binding site of PPAR. At a concentration of 10 , also

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2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridinehydratehydrochloride

(694433-59-5)
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-

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2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE

(905973-89-9)
Ataxia-telangiectasia mutated (ATM) and ATM- and Rad3-related (ATR) kinases mediate the DNA damage response pathway in cells upon encounter with genotoxic agents. Their signaling can activate cell cycle arrest, DNA repair, induction of premature senescence, and cell death. Inhibiting this pathway is one strategy implemented to increase the therapeutic capacity of certain genotoxic anti-cancer regimens by sensitizing cancer cells to these agents. CGK733, a thiourea-containing compound, was origin

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2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzo[d]imidazole

(1255517-76-0)
PF-4708671 is a highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). PF-4708671 inhibits S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect on highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases.

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Small molecule inhibitors are a type of molecules that can interact with proteins and reduce the biological activity of target proteins, including enzyme inhibitors, transcription factor inhibitors, and ion channel blockers. It acts on popular signaling pathways, popular targets and popular research fields: MAPK, PI3K, JAK / STAT and other signaling pathways, HDAC, Aurora kinase, CDK and cell cycle regulators, integrase / protease, etc. Research fields such as epigenetics, CNS, GPCR, anti-virus, antibacterial / anti-inflammatory. It is an effective tool for cell biology research.

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