VVD-118313 | JAK1 inhibitor | Probechem Biochemicals

Chemical Structure : VVD-118313

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VVD-118313 (VVD118313)

货号: PC-49343Not For Human Use, Lab Use Only.

VVD-118313 (VVD118313) is a potent, selective and allosteric inhibitor of the non-catalytic pseudokinase domain of JAK1 (C817), blocks JAK1-dependent trans-phosphorylation and cytokine signaling.

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生物&药学活性

VVD-118313 (VVD118313) is a potent, selective and allosteric inhibitor of the non-catalytic pseudokinase domain of JAK1 (C817), blocks JAK1-dependent trans-phosphorylation and cytokine signaling.

VVD-118313 does not impair JAK2-dependent cytokine signaling and are inactive in cells expressing a C817A JAK1 mutant.

VVD-118313 inhibits IFNα-stimulated STAT1 phosphorylatio with IC50 of 32 nM.

VVD-118313 selectively inhibits JAK1 by engagement of C817.

VVD-118313 potently inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, and IL-2-pSTAT5 pathways in human PBMCs, while sparing JAK2- and TYK2/JAK2-dependent signaling.

VVD-118313 potently inhibits STAT3 phosphorylation in splenocytes from Tyk2−/− mice.

物理化学性质&存储条件

分子量	429.356
分子式	C19H22Cl2N2O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-((S)-3-(3,4-dichlorophenyl)piperidin-1-yl)-3-((R)-1-(methylsulfonyl)pyrrolidin-3-yl)prop-2-yn-1-one

参考文献

1. Kavanagh ME, et, al. Nat Chem Biol. 2022 Dec;18(12):1388-1398.

VVD-118313 (VVD118313)

生物&药学活性

物理化学性质&存储条件

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VVD-118313 (VVD118313)

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