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Key Documents

5.30389

Sigma-Aldrich

GSK′872

≥98% (HPLC), solid, RIPK3 inhibitor, Calbiochem®

別名:

RIPK3 Inhibitor, GSK′872, N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine, RIP3 Kinase Inhibitor I, Receptor-Interacting Protein Kinase 3 Inhibitor I, GSK-872, Necrosis Inhibitor V, RIPK3 Inhibitor I

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About This Item

実験式(ヒル表記法):
C19H17N3O2S2
CAS番号:
分子量:
383.49
UNSPSCコード:
12352200
NACRES:
NA.77

product name

RIPK3 Inhibitor, GSK′872,

アッセイ

≥98% (HPLC)

品質水準

形状

solid

メーカー/製品名

Calbiochem®

保管条件

OK to freeze
protect from light

yellow

溶解性

DMSO: 100 mg/mL

保管温度

2-8°C

詳細

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 µM; Cat. Nos. 480065 & 505224) and genetic knockdown can be employed in conjunction with GSK′872 (3 µM) 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 µM; 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 µM; Cat. Nos. 480065 & 505224) can be employed in conjunction with GSK′872 (3 µM) 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 µM; Cat. Nos. 627609 & 627610).

生物化学的/生理学的作用

Cell permeable: yes
Primary Target
RIP3 Kinase
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


試験成績書(COA)

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文書ライブラリにアクセスする

Lei Wu et al.
Cancer immunology research, 8(5), 710-721 (2020-03-04)
Metabolic reprogramming is critical for the polarization and function of tumor-associated macrophages (TAM) and hepatocarcinogenesis, but how this reprogramming occurs is unknown. Here, we showed that receptor-interacting protein kinase 3 (RIPK3), a central factor in necroptosis, is downregulated in hepatocellular

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