FM-381

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FM-381 (FM381) 是一种有效、特异性、可逆的 JAK3 共价抑制剂，IC50 为 127 pM。

FM-381 (FM381) is a potent, specific, reversible and covalent inhibitor of JAK3 with IC50 of 127 pM, 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and Tyk2, respectively; targets the unique Cys909 at the gatekeeper position +7 in JAK3; blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells.

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 μM.

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FM381 | FM 381

Angiogenesis

JAK

JAK

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2226521-65-7

428.496

C24H24N6O2

>98% (HPLC)

DMSO : 12.8 mg/mL 29.87 mM

O=C(N(C)C)/C(C#N)=C/C(O1)=CC=C1C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5

(E)-2-cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide

(-20℃)

With Ice Pack

≥ 2 years