K02288

1431985-92-0

C20H20N2O4

DMSO : >= 58.6 mg/mL (166.30 mM)

TGF-beta/Smad

K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC₅₀s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC₅₀s of of 5-34 nM. IC50 & Target: IC50:1.8 nM (ALK1), 1.1 nM (ALK2), 34.4 nM (ALK3), 6.3 nM (ALK6), 302 nM (ALK4), 321 nM (ALK5)^[1] In Vitro: K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC₅₀ of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 uM^[1]. K02288 binds to ALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs^[2]. In Vivo: K02288 (1 uM) induces dysfunctional angiogenesis in a chick embryo CAM model^[2].