HTH-01-015 is a potent, specific NUAK1 (AMPK-related kinase 5, ARK5) inhibitor with IC50 of 100 nM, displays >100-fold higher potency than NUAK2.
HTH-01-015 also does not markedly suppress the activity of any of the other 139 protein kinases, including AMPK.
HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation in vivo, the NUAK1 mutation (A195T) renders resistant to HTH-01-015.
HTH-01-015 significantly inhibits migration the proliferation of MEFs (mouse embryonic fibroblasts).
