SGC-GAK-1 是细胞周期蛋白 G 相关激酶 (GAK) 的选择性抑制剂(Ki:3.1 nM)，可用作 GAK 的化学探针。

SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).

SGC-GAK-1 potently binds GAK (Ki: 3.1 nM; Kd: 1.9 nM). SGC-GAK-1 showed strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 μM, but the minimal effect in PC3 and DU145 cells. In dose-response SGC-GAK-1 showed potent antiproliferative activity in LNCaP and 22Rv1 cells at a similar dose range that it engages GAK.

2226517-76-4

C18H17BrN2O3

389.249

SGC-GAK-1

Ethanol:15 mg/mL
DMSO:40 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years