GA-017是一种强效的选择性 LATS1 和 LATS2 (大型肿瘤抑制激酶 1/2) 抑制剂，其 IC50 值分别为 4.10 和 3.92 nM。GA-017 是一种细胞增殖激活剂。GA-017 促进 YAP/TAZ 激活和核转位。GA-017 在 3D 培养条件下促进细胞生长。GA-017 增强小鼠肠道类器官离体的形成。
货号:ajcx38946
CAS:2351906-74-4
分子式:C18H21N3O4
分子量：343.38
溶解度:DMSO : 20.83 mg/mL (60.66 mM; ultrasonic and warming and heat to 80°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.