GA-017 (E1145-GRP)

GA-017 inhibits the serine/threonine protein kinases large tumor suppressor kinase 1/2 (LATS1/2), which exerts inhibitory with IC50s against LATS1 and 2 of 4.10±0.79 and 3.92±0.42 nM, respectively, and competitively inhibits LATS1 and 2 against ATP, with Ki (inhibition constant) values of 0.58±0.11 and 0.25±0.03 nM, respectively.