RIPK3 Inhibitor, GSK'872-Calbiochem

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一般描述

A cell-permeable quinolinyl-benzothiazolamine compound that is reported to act as a RIP3-selective kinase inhibitor with >1,000-fold selectivity over a vast majority of more than 300 other kinases, including RIP1. RIP1 inhibitor Nec-1 (30 ?M; Cat. Nos. 480065 & 505224) and genetic knockdown can be employed in conjunction with GSK′872 (3 ?M) in delineating RIP1- vs. RIP3-dependency in Toll-like receptors- (TLRs) mediated necrosis and TNFR1-initiated necroptosis in the presence or absence of caspase inhibitor Z-VAD-FMK (25 ?M; Cat. Nos. 627609 & 627610). While RIP3 and its downstream substrate MLKL are shown to mediate TLR3-initiated necrosis in the presence of Z-VAD-FMK in murine macrophage (BMDM & J774), fibroblast (3T3-SA & MEF), and endothelial (SVEC4-10) cultures, only in BMDM & J774 macrophage cultures is RIP1 involvement also seen in TLR3-mediated necrosis.
A cell-permeable quinolinyl-benzothiazolamine compound that is reported to act as a RIP3-selective kinase inhibitor with >1,000-fold selectivity over a vast majority of more than 300 other kinases, including RIP1. RIP1 inhibitor Nec-1 (30 ?M; Cat. Nos. 480065 & 505224) can be employed in conjunction with GSK′872 (3 ?M) in delineating RIP1- vs. RIP3-dependency in Toll-like receptors- (TLRs) mediated necrosis and TNFR1-initiated necroptosis in the presence or absence of caspase inhibitor Z-VAD-FMK (25 ?M; Cat. Nos. 627609 & 627610).

生化/生理作用

Cell permeable: yes
Primary Target
RIP3 Kinase
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Kaiser, W.J., et al. 2013.J. Biol. Chem.288,31268.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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