Chemical Name: N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
Biological ActivityPotent and selective receptor activating protein kinase 3 (RIP3) inhibitor (IC50 = 1.3 nM). Exhibits >1000-fold selectivity for RIP3 over a panel of 300 other kinases including RIP1. Inhibits TNF-induced cell death in 3T3-SA cells and TLR3-induced necrosis in fibroblasts in vitro. Blocks necroptosis of primary human neutrophils from whole blood. Also induces apoptosis at higher concentrations (3 - 10 μM).
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Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL.
Kaiser et al.
RIP3 induces apoptosis independent of pronecrotic kinase activity.
Mandal et al.
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Working concentration using 10 nM for different incubation time in HT-29 cells and the cell death rate was measured.
used to inhibit ripk3 kinase activity to block necroptosis