GRK5-IN-3 是 G 蛋白偶联受体激酶 5 (GRK5) 的共价抑制剂。GRK5-IN-3 对GRK5和GRK6有显著的抑制作用，IC50分别为 0.22 μM 和 0.41 μM。

GRK5-IN-3 is a covalent inhibitor of GRK5 ( G Protein-Coupled Receptor Kinase 5 ). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC 50 s of 0.22 μM and 0.41 μM, respectively [1].

GRK5 can be used to cancer, neurodegeneration, type 2 diabetes, heart failure and cardiovascular (CVD) research [1]. GRK5-IN-3 (Compound 5) (0-333 μM; 0-4 h) inhibits GRK5 in a time-dependent manner with IC 50 s of 59 μM (0 h), 11.3 μM (0.5 h), 6.2 μM (1 h), and 0.22 μM (4 h), respectively [1]. GRK5-IN-3 (0-333 μM; 0-4 h) also shows selectivity to human GRK5 over bovine GRK2 and bovine GRK1, with IC 50 s >100 μM (GRK1/2), respectively [1]. GRK5-IN-3 (0-333 μM; 0-4 h) exerts inhibition against GRK5, while light activated ROS as substrate, with IC 50 s of >100 μM (0 h), 4.2 μM (0.5 h), 3.4 μM (1 h), and 0.9 μM (4 h), respectively [1]. GRK5-IN-3 (0-333 μM; 4 h) shows no inhibitory effect on mutant GRK5 (GRK5-C474S, Cys474 mutated to serine), with IC 50 values >100 μM [1].

2410793-22-3

C23H21N7O3

443.46

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years