A potent JAK3 inhibitor
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FM-381

Item No. 23204

Technical Information
Formal Name
2-cyano-3-[5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-2-furanyl]-N,N-dimethyl-2-propenamide
CAS Number
2226521-65-7
Molecular Formula
C24H24N6O2
Formula Weight
Purity
≥98%
A crystalline solid
λmax
240, 370 nm
SMILES
O=C(N(C)C)/C(C#N)=C/C1=CC=C(C2=NC3=C(C(C=CN4)=C4N=C3)N2C5CCCCC5)O1
InChi Code
InChI=1S/C24H24N6O2/c1-29(2)24(31)15(13-25)12-17-8-9-20(32-17)23-28-19-14-27-22-18(10-11-26-22)21(19)30(23)16-6-4-3-5-7-16/h8-12,14,16H,3-7H2,1-2H3,(H,26,27)/b15-12+
InChi Key
GJMZWYLOARVASY-NTCAYCPXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    FM-381 is a potent inhibitor of JAK3 (IC50 = 127 pM).1 It is 400-, 2,700-, and 3,600-fold selective for JAK3 over JAK1, JAK2, and TYK3 and only inhibits 11 kinases by less than 50 percent in a panel of 410 kinases when used at a concentration of 500 nM. FM-381 (1 μM) blocks JAK3-dependent STAT5 phosphorylation but not JAK3-independent STAT3 signaling in IL-2- and IL-6-stimulated T cells, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Forster, M., Chaikauad, A., Bauer, S.M., et alSelective JAK3 inhibitors with covalent reversible binding mode targeting new induced fit binding pocket. Cell Chem. Biol. 23(11), 1335-1340 (2016).