DATASHEET
Formulation
White solid
Storage:
-20°C
Product Information:
SGC-GAK-1 is a highly potent and selective inhibitor of cyclin G associated kinase (GAK), a member of the numb-associated kinase (NAK) family involved in membrane trafficking and sorting of proteins and is required for the maintenance of centrosome maturation and progression though mitosis. KD = 1.9 nM with >50-fold selectivity against a panel of 400 kinases. It also displayed affinity for RIPK2 (KD = 110 nM) and ADCK3 (KD = 190 nM). SGC-GAK-1 displayed potent cellular activity in HEK293T cells (IC50 = 120 nM) and showed strong growth inhibition in the prostate cancer cell lines LNCaP (IC50 = 0.65 µM) and 22Rv1 (IC50 = 0.17 µM).
Description:
CAS Number: 2226517-76-4<br></br>Chemical Name: 6-Bromo-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine<br></br>Molecular weight: 389.25<br></br>Formula: C18H17BrN2O3 <br></br>Solubility: DMSO (>25 mg/ml) Ethanol (10 mg/ml)<br></br>Physical Properties: Pale yellow solid<br></br>Purity: 99% by HPLC NMR (Conforms)