compound introduction
GSK180736A (GSK180736) 是一种Rho相关的、含卷曲螺旋（coiled-coil）的蛋白激酶抑制剂，与GRK2(G protein-coupled receptor kinase 2)结合，logIC50为-6.6。对GRK2的选择性比对GRK1和GRK5高400倍以上。 Information GSK180736A (GSK180736) GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5. Targets ROCK (Cell-free assay); GRK2 (Cell-free assay) 100 nM; 6.6(pIC50) In vitro GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).
