GSK547

GSK547 is a preclinical, orally bioavailable small-molecule inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), designed by GSK as a highly selective tool compound with improved pharmacokinetics over earlier RIPK1 inhibitors for chronic in vivo studies. It potently and selectively blocks RIPK1 kinase activity, thereby inhibiting RIPK1-dependent necroptosis and inflammatory signaling, reducing macrophage-mediated adaptive immune tolerance and pro‑inflammatory cytokine production in multiple models. In preclinical studies, GSK547 showed antitumor and immunomodulatory activity in pancreatic ductal adenocarcinoma when combined with immune checkpoint blockade, and demonstrated anti‑inflammatory effects in T cell–dependent colitis and atherosclerosis models, supporting its use as a chemical probe and potential lead for cancer, neurodegenerative, and inflammatory indications.

Other names

RIP1 inhibitor GSK547RIP-1 inhibitor GSK547RIP 1 inhibitor GSK547