Chemical Structure : R191
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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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.
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外观性状 | Solid | |
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Solubility |
10 mM in DMSO |
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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