YYSW001 | JAK1 inhibitor | Probechem Biochemicals

Chemical Structure : YYSW001

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YYSW001 (YYSW-001)

货号: PC-26418Not For Human Use, Lab Use Only.

YYSW001 is a potent, highly selective and orally bioavailable JAK1 inhibitor with IC50 of 6 nM, with no activity against JAK2 and JAK3.

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生物&药学活性

YYSW001 is a potent, highly selective and orally bioavailable JAK1 inhibitor with IC50 of 6 nM, with no activity against JAK2 and JAK3.
YSW001 potently inhibits IL-4-induced STAT6 phosphorylation (JAK1-STAT6, IC50 =0.041 μM) while showing markedly weaker inhibitory potency of GM-CSF-induced STAT5 phosphorylation (JAK2-STAT5 IC50 =5.530 μM) in cellular pathway inhibition assays.
YSW001 demonstrates superior JAK1/JAK2 selectivity profiles at both enzymatic and cellular levels, markedly outperforming upadacitinib and filgotinib.
YYSW001 exhibits potent inhibitory activity against JAK1 (IC50 = 290.2 nM), with negligible inhibition against JAK2, JAK3, and TYK2 (IC50 > 10000.0 nM) in JAK subtypes in Ba/F3-engineered cell lines.
YYSW001 dose-dependently inhibits STAT3 phosphorylation in both CD3+ T cells and CD14+ monocytes (IC50 = 7065.0 nM and 3001.0 nM) in IL-6-induced STAT3 phosphorylation assays, with minimal inhibitory effects on STAT5 phosphorylation in CD14+ monocytes and CD33+ granulocytes.
YSW001 demonstrates therapeutic efficacy comparable to upadacitinib in rat model of collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models.

物理化学性质&存储条件

分子量	417.38
分子式	C18H20F5N5O
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	(R)-1-(1-((S)-1-(3,3,4,4,4-Pentafluorobutyl)pyrrolidin-3-yl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)ethan-1-ol

参考文献

1. Kaiyong Hu, et al. J Med Chem. 2026 Mar 19. doi: 10.1021/acs.jmedchem.5c03183.

YYSW001 (YYSW-001)

生物&药学活性

物理化学性质&存储条件

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YYSW001 (YYSW-001)

生物&药学活性

物理化学性质&存储条件

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