2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
SGC-GAK-1 (GAK inhibitor 1) is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki of 3.2 nM, 16,000-fold selectivity over NAK; SGC-GAK-1 is highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target; shows high affinity for GAK in cells in cellular target engagement assays (IC50=120 nM), 3-fold selectivity over RIPK2 in cells (IC50=360 nM); robustly blocked growth of 22Rv1 and LNCaP cell lines (Viability IC50=0.17 and 0.65 uM) that express AR splice variants associated with poor clinical prognosis, treatment of 22Rv1 cells with led to PARP cleavage, a marker of cells undergoing apoptosis, and an increase in phosphorylated histone H3 Ser10, as had been observed in with GAK targeting siRNA.
