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GRK5-IN-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GRK5-IN-3图片
CAS NO:2410793-22-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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GRK5GRK6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].

分子量

443.46

Formula

C23H21N7O3

CAS 号

2410793-22-3

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.