HTH01-015

HTH01-015 (also referred to as HTH-01-015) is a potent and highly selective small molecule inhibitor of NUAK family kinase 1 (NUAK1, also known as ARK5), with an IC50 of approximately 100 nM. Developed through a collaboration between the Dana-Farber Cancer Institute and the University of Dundee, HTH01-015 exhibits greater than 100-fold selectivity for NUAK1 over the closely related isoform NUAK2 (IC50 > 10 µM) and shows no significant off-target activity against a panel of 139 other kinases. In vitro, HTH01-015 suppresses NUAK1-mediated phosphorylation of myosin phosphatase-targeting subunit 1 (MYPT1) at Ser445, thereby inhibiting cell migration, proliferation, and invasion. It is primarily utilized as a research-use-only tool compound to investigate the physiological roles of NUAK1 in processes such as cancer progression, cell adhesion, and smooth muscle contraction.

Other names

HTH 01-015HTH01-015HTH-01-015HTH-01015HTH01015HTH 01015