GSK547

  • Chemical Properties
CAS No. 2226735-55-1 Cat. No. BCP30590
Name GSK547
Synonyms GSK-547; GSK 547; RIP1i;
Formula C20H18F2N6O M. Wt 396.40
  • Biological Activity
Description GSK547 (RIP1i, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo; exhibited a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963; reprogrammed TAMs toward an MHCIIhiTNFα+IFNγ+ immunogenic phenotype in a STAT1-dependent manner. RIP1 inhibition in TAMs resulted in cytotoxic T cell activation and T helper cell differentiation toward a mixed Th1/Th17 phenotype, leading to tumor immunity in mice and in organotypic models of human Pancreatic ductal adenocarcinoma (PDA).
Pathways Apoptosis Pathway 
Targets RIP 

Structure

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