Drug intelligence / Profile preview

GSK'872

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Experimental (mainly In Vitro/in Vivo Preclinical Studies)
01

Overview

GSK'872 is a potent and selective small molecule inhibitor of **receptor-interacting serine/threonine-protein kinase 3 (RIPK3)**, with an IC50 in the low nanomolar range (1.3–1.8 nM)[1][5][7][14]. Developed originally by GSK, this compound exhibits over 1000-fold selectivity for RIPK3 over other kinases, including RIPK1, and effectively blocks necroptosis (programmed necrotic cell death) and TNF- or virus-induced necrosis in vitro[1][5][7][12][14]. At higher concentrations, GSK'872 can paradoxically induce apoptosis via the formation of a caspase 8-dependent complex involving RIPK3 and RIPK1[2][13]. It has demonstrated neuroprotective and anti-inflammatory effects in preclinical models, including those of Parkinson's disease, retinal degeneration, traumatic brain injury, and chronic obstructive pulmonary disease by inhibiting necroptosis- and inflammation-mediated pathways[4][6][9][10]. GSK'872 is primarily used as a chemical probe in cell and animal studies and is not an approved therapeutic agent.

Other names
N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amineRIP3 Kinase Inhibitor IRIP-3 Kinase Inhibitor IRIP 3 Kinase Inhibitor IReceptor-Interacting Protein Kinase 3 Inhibitor INecrosis Inhibitor VRIPK3 Inhibitor IRIPK-3 Inhibitor IRIPK 3 Inhibitor I
02

Targets

RIPK3

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