CID24856225
| 中文名称 | CID24856225 |
|---|---|
| 中文同义词 | PME-1抑制剂(ABL127);化合物 T14084;化合物 ABL127;1073529-41-5;ABL127 |
| 英文名称 | CID24856225 |
| 英文同义词 | (3R)-1,2-Dicarboxylic acid, 3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine 1,2-dimethyl ester;(3R)-Dimethyl 3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine-1,2-dicarboxylate;ABL127;CID24856225;4-OXO-3,3-DIPHENYL-[1,2]DIAZETIDINE-1,2-DICARBOXYLIC ACID DIMETHYL ESTER(WX619174);ABL127 (AB L127;ML174);1,2-Diazetidine-1,2-dicarboxylic acid, 3-cyclopentyl-4-oxo-3-phenyl-, 1,2-dimethyl ester, (3R)- |
| CAS号 | 1073529-41-5 |
| 分子式 | C17H20N2O5 |
| 分子量 | 332.35 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;制剂-抑制剂 |
| Mol文件 | 1073529-41-5.mol |
| 结构式 |  |
CID24856225 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 |
| 形态 | 膜状 |
| 酸度系数(pKa) | -3.45±0.40(Predicted) |
| 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 |
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.
安全信息
| WGK Germany | 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-108317 | ABL127 | 1073529-41-5 | 1 mg | 1704元 |
| 2025/12/22 | HY-108317 | CID24856225 ABL127 | 1073529-41-5 | 5mg | 3750元 |