selonsertib

Selonsertib (GS-4997) 是一种选择性的，具有生物口服可利用的凋亡信号调节激酶1 抑制剂，pIC50为 8.3。它具有潜在的抗炎、抗肿瘤和抗纤维化活性。

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

VU0466551 is a selective activator of homomeric G protein gated, inwardly rectifying, potassium subunit 1 (GIRK1) channels.