Catalog No.: PC-35852Not For Human Use, Lab Use Only.
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 (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.
SGC-GAK-1 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).
SGC-GAK-1 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.
