GSK180736A 是 Rho 相关卷曲螺旋激酶 1 (ROCK1) 抑制剂，IC50值为 100 nM。它也是选择性的ATP-竞争性 G 蛋白偶联受体激酶 2 抑制剂，IC50值为 0.77 μM，其选择性比其他 GRK 高 100 倍以上。

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5[2]. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM)[3].

Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1].

817194-38-0

C19H16FN5O2

365.368

GSK180736

Ethanol:3 mg/mL (8.21 mM)
H2O:<1 mgml
DMSO:68 mg/mL (186.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years