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FM-381

CAS No. : 2226521-65-7

MCE 站：FM-381

产品活性：FM-381 是有效，共价，可逆的 JAK3 抑制剂，靶向 Cys909 位点。FM-381 对 JAK3 的 IC₅₀ 值为127 pM，选择性分别比 JAK1，JAK2 和 TYK2 高 410，2700 和 3600 倍。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: FM-381 is screened against a panel of 410 kinases at concentrations of 100 nM and 500 nM. FM-381 has no relevant effect on the activity of any tested kinases except JAK3 at a concentration of 100 nM. At 500 nM, FM-381 moderately inhibits 11 other kinases besides JAK3 with residual activities below 50%. FM-381 is found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 selectively inhibits JAK3 signaling in human CD4⁺ T Cells. FM-381 shows an apparent EC₅₀ of 100 nM in a dose dependent BRET assay and blocks IL2 stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6 (JAK1/2/TYK dependent) stimulated STAT3 signalling in human CD4⁺ T cells up to 1 ?M.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Chemical Probe Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Gandotinib  |  Lestaurtinib  |  Cucurbitacin I  |  Oclacitinib maleate  |  JANEX-1  |  XL019  |  Atractylenolide I  |  FLLL32  |  LFM-A13  |  Brevilin A  |  ZM39923 hydrochloride  |  Ginsenoside Rk1  |  WHI-P154  |  Curculigoside  |  RO8191  |  Reticuline  |  TCS 21311  |  WHI-P97  |  Coumermycin A1  |  Delphinidin chloride  |  Ilginatinib maleate  |  Protosappanin A  |  Dehydrocrenatidine  |  FM-479  |  NSC 33994  |  ZM 449829

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