1073529-41-5
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
| 沸点 | 422.8±48.0 °C(Predicted) |
| 密度 | 1.330±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥5mg/mL |
| 酸度系数(pKa) | -3.45±0.40(Predicted) |
| 形态 | film |
| 颜色 | 无色 |
| InChI | 1S/C17H20N2O5/c1-23-15(21)18-14(20)17(13-10-6-7-11-13,19(18)16(22)24-2)12-8-4-3-5-9-12/h3-5,8-9,13H,6-7,10-11H2,1-2H3/t17-/m0/s1 |
| InChIKey | ZRHWCAFAIHTQKD-KRWDZBQOSA-N |
| SMILES | O=C1[C@](C2=CC=CC=C2)(C3CCCC3)N(C(OC)=O)N1C(OC)=O |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
| WGK Germany | 3 |
| 存储类别 | 11 - Combustible Solids |
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.