GA-017是一种有效的选择性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 是细胞增殖的激活剂。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的离体形成。
产品描述
GA-017 is a potent and selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1/2), with IC 50 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].
体外活性
GA-017 suppresses the HUVECs cell death and promotes their cell growth [1]. GA-017 facilitates SKOV3 cell growth, with an EC 50 of 3.51 ± 0.26 μM [1]. GA-017 competitively inhibited LATS1 and 2 against ATP, with K i (inhibition constant) values of 0.58 ± 0.11 and 0.25 ± 0.03 nM, respectively [1].
Cas No.
2351906-74-4
分子式
C18H21N3O4
分子量
343.38
储存和溶解度
DMSO:18.9mg/mL (55mM),ultrasonic and warming and heat to 80°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years