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FM-381

Chemical Structure : FM-381

CAS No.: 2226521-65-7

FM-381 (FM381;FM 381)

Catalog No.: PC-63575Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
FM-381 targets the unique Cys909 at the gatekeeper position +7 in JAK3.
FM-381 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.

Physicochemical Properties

M.Wt 428.496
Formula C24H24N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Forster M, et al. Cell Chem Biol. 2016 Nov 17;23(11):1335-1340.

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