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首页-小分子抑制剂&激动剂-Immunology/Inflammation-IRAK-R191
R191

Chemical Structure : R191

CAS No.:

R191 (R-191)

货号: PC-35595Not For Human Use, Lab Use Only.

R191 (R-191) is a potent, small molecule IRAK1/4 kinase inhibitor (IRAK4 IC50=3 nM), exhibits good selectivity against a broad panel of kinases.

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

    生物&药学活性

    R191 (R-191) is a potent, small molecule IRAK1/4 kinase inhibitor (IRAK4 IC50=3 nM), exhibits good selectivity against a broad panel of kinases.
    R191 blocks TLR- and IL-1R-induced cytokine production in primary cells with potencies below 50nM while sparing unrelated pathways with at least 20-fold window.
    R191 potently inhibits expression of PD-L1, potentially promoting recognition of AML blasts by the immune system in multiple AML lines.
    R191 exhibits strong synergy with Bcl2 and BCR pathway inhibitors against a number of DLBCL lines in vitro; also decreases serum IL-6 in an acute mouse model of IL-1β-induced cytokine release and blocks joint inflammation in the collagen-induce arthritis model.

    物理化学性质&存储条件

    分子量
    分子式
    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

    参考文献

    1. Ni H, et al. Clin Cancer Res. 2018 Aug 20. pii: clincanres.3265.2017.

    2. Vadim V. Markovtsov, et al. Abstract 346: Potential role for R191, potent and selective IRAK4 kinase inhibitor, in treatment of hematologic malignancies. AACR 2016.

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