RIPK3 INHIBITOR GSK'872 (C15-1305-013)

General description

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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
RIP3 Kinase

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 383.49. Empirical Formula: C₁₉H₁₇N₃O₂S₂. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.