GSK-269962A

GSK‑269962A is a potent and selective small molecule inhibitor of Rho-associated protein kinases (ROCK), specifically targeting both ROCK1 and ROCK2 isoforms with IC50 values of 1.6 nM and 4 nM respectively[1][9][7]. It displays over 30-fold selectivity for ROCK compared to other serine/threonine kinases[9]. Mechanistically, it inhibits the ROCK/c-Raf/ERK signaling pathway. Preclinical studies have shown that GSK‑269962A induces cell cycle arrest in the G2 phase and promotes apoptosis in acute myeloid leukemia (AML) cells by downregulating key cell cycle regulatory proteins such as Cyclin B1-Cdc2 complex components[5][6]. The compound also exhibits anti-inflammatory and vasodilatory effects; it induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM), lowers blood pressure in hypertensive rat models[7][9], and has been used experimentally to study cardiovascular disease mechanisms. Developed by GlaxoSmithKline (GSK), it is currently considered an investigational tool compound for research purposes only.

Other names

N-(3-((2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin–6–yl)oxy)phenyl)-4-(2-(4-morpholinyl)ethoxy)benzamideBenzamide, n-(3–((2–(4-amino–1,2,5–oxadiazol–3–yl)–1–ethyl–1h-imidazo(4,5-c)pyridin−6−yl)oxy)phenyl)-4-(2-(4-morpholinyl)ethoxy)