SGC-GAK-1

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK[1].

SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with Kis of 3.1 nM, 53 µM, 51 µM, respectively[1].SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with KDs of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively[1].SGCGAK-1 (0.1, 1, and 10 µM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 µM, but minimal effect in PC3 and DU145 cells[1].|| Cell Viability Assay[1]||Cell Line:|Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145) |Concentration:|0.1, 1, and 10 µM|Incubation Time:|48 hours or 72 hours|Result:|Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50s of 0.05±0.15 µM and 0.17±0.65 µM, respectively.

[1]. Asquith CRM, et al. SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). J Med Chem. 2019 Feb 26.