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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Hippo-GA-017
GA-017

Chemical Structure : GA-017

CAS No.: 2351906-74-4

GA-017 (GA017)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 343.383
分子式 C18H21N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

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

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