Inhibitor of receptor interacting serine/threonine kinase 1
Product Description
Information
GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
Targets
RIP1 kinase (Cell-free assay) 6.3 nM
In vitro
GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinasedependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor is also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.
1.Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU et al.. (2019) Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.. ACS Med Chem Lett, 10 (6):(857-862). [PMID:31223438]
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I2216048