GA-017 (GA017) is a potent, selective, ATP-competitive LATS kinase (LATS1/2) inhibitor with IC50 of 4.10/3.92 nM, respectively, promotes cell growth.GA-017 increases the number and size of spheroids of various cell-types in both scaffold-based and scaffold-independent cultures.GA-017 also enhances the ex vivo formation of mouse intestinal organoids.GA-017 facilitates the growth of spheroids and organoids by stabilizing and translocating YAP/TAZ into the cell nucleus.GA-017 inhibits the Hippo pathway to promote YAP/TAZ stabilization and nuclear translocation.GA-017 induces expression of Hippo pathway-related genes such as ANKRD1, CYR61, and CTGF in SKOV3 cells in a time- and dose-dependent manner.GA-017 inhibited the activity of 16 kinases of the AGC family at 100 nM against a panel of 321 diverse kinases.The serine/threonine protein kinases LATS (LATS1/2) phosphorylate YAP/TAZ, key effectors of the growth- and proliferation-regulating Hippo signaling pathway.
Cat.No
DC70423
Name
GA-017
Chemical Properties
CAS
2351906-74-4
Formula
C18H21N3O4
MW
343.383
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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