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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-RI-962
RI-962

Chemical Structure : RI-962

CAS No.: 2763831-53-2

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RI-962 (RI962)

货号: PC-49455Not For Human Use, Lab Use Only.

RI-962 (RI 962) is a potent and selective RIPK1 inhibitor with IC50 of 5.9 nM in ADP-Glo assays.

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

    生物&药学活性

    RI-962 (RI 962) is a potent and selective RIPK1 inhibitor with IC50 of 5.9 nM in ADP-Glo assays.
    RI-962 shows little to no activity against a panel of 408 human kinases (IC50>10 μM) except MLK3 (IC50=3.75 μM, 107-fold less potent against MLK3 than against RIPK1).
    RI-962 occupies both the ATP-binding pocket and the allosteric site simultaneously, indicating a type II kinase inhibitor.
    RI-962 exerted a dose-dependent protective effect against necroptotic death, with EC50 values of 10.0, 4.2, 11.4, and 17.8 nM for HT29, L929, J774A.1, and U937 cells, respectively.
    RI-962 inhibited TSZ-induced necroptosis and improved cell survival in a concentration-dependent manner, which is more potent than positive control GSK3145095.
    RI-962 markedly inhibited the phosphorylation of RIPK1 and its downstream signaling proteins RIPK3 and MLKL in a dose-dependent manner.
    RI-962 (40 mg/kg, i.v.) remarkably reduced the TNFα-induced systemic inflammatory response syndrome (SIRS), and the concentrations of proinflammatory cytokines (IL-1β and IL-6) in mice.
    RI-962 reduced inflammation in acute DSS-induced colitis, reduced the levels of pRIPK1, pRIPK3, and pMLKL proteins in the colon during DSS challenge, but did not impact the expression of RIPK1, RIPK3, and MLKL proteins.

    物理化学性质&存储条件

    分子量 480.572
    分子式 C28H28N6O2
    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

    5-(2-isobutyramido-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1-methyl-N-(1-phenylethyl)-1H-indole-3-carboxamide

    参考文献

    1. Yueshan Li, et al. Nat Commun. 2022 Nov 12;13(1):6891.

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