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GA-017

Chemical Structure : GA-017

CAS No.: 2351906-74-4

GA-017 (GA017)

Catalog No.: PC-73093Not For Human Use, Lab Use Only.

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 343.383
Formula C18H21N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-2-(1-(2,4-dihydroxy-3-methylphenyl)propylidene)-N-(3-hydroxybenzyl)hydrazine-1-carboxamide

References

1. Aihara A, et al. J Biol Chem. 2022 Feb 26:101779.

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