1073529-41-5
1073529-41-5 结构式
基本信息
ML174)
CID24856225
ABL127 (AB L127
ABL127 >=98% (HPLC)
(3R)-Dimethyl 3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine-1,2-dicarboxylate
4-OXO-3,3-DIPHENYL-[1,2]DIAZETIDINE-1,2-DICARBOXYLIC ACID DIMETHYL ESTER(WX619174)
(3R)-1,2-Dicarboxylic acid, 3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine 1,2-dimethyl ester
1,2-Diazetidine-1,2-dicarboxylic acid, 3-cyclopentyl-4-oxo-3-phenyl-, 1,2-dimethyl ester, (3R)-
物理化学性质
常见问题列表
IC50: 6.4 nM (PME-1 in HEK293T), 4.2 nM (PME-1 in MDA-MB-231)
Three described PME-1 inhibitors are tested in this assay and a thermal shift with 100 μM ABL127 is detected. Using 25 or 50 μM ABL127 also shows a shift in protein melting temperature. It is found that treatment of Ishikawa cells with ABL127 and AMZ-30 significantly decreases cell proliferation similarly to depletion of PME-1 with shRNA. It is also found that treatment of ECC-1 cells with ABL127 or AMZ-30 affects cell invasion in a dose-dependent manner. The treatment of EC cells with ABL127 leads to a significant ~45 % increase in protein phosphatase 2A (PP2A) activity, while treatment with AMZ-30 leads to a modest ~10 % increase in PP2A activity.
No significant decrease in tumor burden can be assessed in these pilot studies. Gel-based profiles indicate that brain PME-1 is inactivated by ABL127, but overlapping serine hydrolase activities preclude a confident assessment of the extent of inactivation.