GSK3145095 (GSK 3145095) is a potent, selective RIP1 Kinase (RIPK1) inhibitor with IC50 of 6.3 nM.
GSK3145095 displays >1500-fold selectivity window at Reaction Biology Corp (359 kinases) and a competition binding assay KINOMEscan at DiscoveRx Corp (456 kinases).
GSK3145095 binds an allosteric pocket at the back of the ATP binding site.
Necroptosis pathway is activated through stimulation with TNF coincubated with the caspase inhibitor QVD-Oph or zVAD.fmk, and the SMAC mimetic RMT 5265, GSK3145095 is very potent as measured by inhibition of cytokine MIP-1β ((IC50=5 nM).
GSK3145095 promoted a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.
