Hydrazinecarboxamide, 2-[1-(2,4-dihydroxy-3-methylphenyl)propylidene]-N-[(3-hydroxyphenyl)methyl]-

Biological Activity

GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids[1]. GA-017 suppresses the cell death of HUVECs and promotes their cell growth[1].GA-017 facilitates SKOV3 cell growth, with an EC50 of 3.51 ± 0.26 μM[1].GA-017 competitively inhibited LATS1 and 2 against ATP, with Ki (inhibition constant) values of 0.58 ± 0.11 and 0.25 ± 0.03 nM, respectively[1].

References

[1]. Aihara A, et al. Small molecule LATS kinase inhibitors block the Hippo signaling pathway and promote cell growth under 3D culture conditions. J Biol Chem. 2022 Apr;298(4):101779.