BQU57 is a Ral inhibitor which can reduced the activation of RalA without effect on the binding of GTP or GDP to RalA. Treatment with BQU57 at concentration<10μM for 2-4 weeks dose-dependently inhibited the anchorage-independent colony formation of Ral-dependent lines, H2122 and H358. Administration of BQU57 at doses of 20mg/kg or 50mg/kg, i.p., inhibited the growth of H2122 tumour xenografts, with decreased activity of RalA and RalB (measured using the respective pull-down assay for each GTPase) in tumor.
作用机制
BQU57 may bind to the guanine nucleotide binding pocket in RalA–GDP.[1]
BQU57 细胞实验
Cell Line
Concentration
Treated Time
Description
References
H2122, H358, H460, and Calu6 human lung cancer cells
10 μM
3 h
Evaluate the effect of compounds on anchorage-independent growth, RBC8 and BQU57 inhibited soft agar colony formation in Ral-dependent cell lines H2122 and H358
Nature. 2014 Nov 20;515(7527):443-7.
Wild-type and caveolin−/− mouse embryonic fibroblasts (MEFs)
15 μM
1 h
Evaluate the effect of compounds on cell spreading, RBC6, RBC8, and RBC10 inhibited cell spreading only in WT MEFs
Nature. 2014 Nov 20;515(7527):443-7.
J82 human bladder cancer cells
50 μM
1 h
Evaluate the effect of compounds on RalA activity, RBC6, RBC8, and RBC10 reduced the activation of RalA
搜索
