FM-381是JAK3的特异性抑制剂，抑制作用具有可逆性，与JAK3共价结合，IC50为127 pM。对JAK3的选择性分别是对JAK1、JAK2、TYK2的400倍、2700倍、3600倍。 Information FM-381 is aJAK3specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. Targets JAK3 (Cell-free) 127 pM In vitro FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper (GK) position +7 in JAK3 exhibited apparent JAK3 IC50 values of 0.127 nM, with 400-, 2700- and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively. FM-381 was found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). 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-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells up to 1 µM. Cell Research(from reference) Cell lines：CD4+ T Cell Concentrations：0, 10, 50, 100, 300 nM Incubation Time：1 h
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FM-381
CAS number：2226521-65-7 molecular formula：C24H24N6O2
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Specs
| Chinese alias | - | ||
| English alias | (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 | ||
| CAS number | 2226521-65-7 | molecular formula | C24H24N6O2 |
| molecular weight | 428.49 g/mol | Exact mass | ≥98% |
| PSA | 104.000 Ų | logp | 4.084 |
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