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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-YYSW001
YYSW001

Chemical Structure : YYSW001

CAS No.: 2763672-36-0

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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    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.
    YYSW001 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.

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