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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-Zharp1-211
Zharp1-211

Chemical Structure : Zharp1-211

CAS No.: 2258671-41-7

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Zharp1-211

货号: PC-49449Not For Human Use, Lab Use Only.

Zharp1-211 is a potent, selective, type II inhibitor of RIPK1 kinase with IC50 of 53 nM and binding Kd of 8.7 nM.

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

    生物&药学活性

    Zharp1-211 is a potent, selective, type II inhibitor of RIPK1 kinase with IC50 of 53 nM and binding Kd of 8.7 nM.
    Zharp1-211 targets the ATP-binding pocket in RIPK1's inactive DLG (Asp156–Leu157–Gly158)-out kinase conformation.
    Zharp1-211 is selective for RIPK1 kinase, does not inhibit RIPK3 and a panel of 468 kinases at 10 uM.
    Zharp1-211 is highly potent for blocking TNF-induced necroptosis in human colon cancer HT-29 cells (EC50=4.6 nM).
    Zharp1-211 efficiently inhibited p-RIPK1 and p-MLKL and necroptosis in intestinal organoids exposed to necroptotic stimuli.
    Zharp1-211 also significantly reduced the transcription of Cxcl9, Cxcl10, CIITA, and H2-DMB1 as well as the expression of MHCII protein in IFN-γ-stimulated mouse intestinal organoids.
    Zharp1-211 treatment (5mg/kg) significantly reduced the severity of graft-versus-host disease (GVHD), leading to improved overall survival rates, ameliorated haplo- identical B6 anti-BDF1 mouse model of GVHD, reduced GVH inflammation in the colon, small intestine, and liver and attenuated skin inflammation.

    物理化学性质&存储条件

    分子量 447.495
    分子式 C24H25N5O4
    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

    tetrahydro-2H-pyran-4-yl 6-(2-(cyclopropanecarboxamido)imidazo[1,2-a]pyridin-6-yl)-2,3-dihydro-1H-pyrrolo[3,2-b]pyridine-1-carboxylate

    参考文献

    1. Xiaoliang Yu, et al. Blood. 2022 Nov 10;blood.2022017262.

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