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。
生物活性 | GRK5-IN-3 is a covalent inhibitor ofGRK5(G Protein-Coupled Receptor Kinase5). GRK5-IN-3 shows potent inhibitory effect toGRK5andGRK6withIC50s of 0.22 μM and 0.41 μM, respectively[1]. |
IC50& Target | IC50: 0.22 μM (GRK5), 0.41 μM (GRK6)[1] |
体外研究 (In Vitro) | 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 IC50s 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 IC50s >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 IC50s 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 IC50values >100 μM[1].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |