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ABL127  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于DMSO(≥5mg/mL)
产品描述：基本信息 产品编号： A12825 产品名称： ABL127 CAS: 1073529-41-5   储存条件 粉末 -20℃ 四年     分子式： C17H20N2O5 溶于液体 -80℃ 六个月 分子量 332.35 -20℃ 一个月 化学名：  (3R)-Dimethyl3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine-1,2-dicarboxylate   生物活性 产品描述 一个有选择且共价的蛋白质甲基酯酶 1 (PME-1) 抑制剂，在 HEK293T 和 MDA-MB-231 细胞中的 IC50 值分别为 6.4 和 4.2nM。 靶点 IC50: 6.4nM (PME-1 in HEK293T), 4.2nM (PME-1 in MDA-MB-231) 体外研究 Three described PME-1 inhibitors are tested in this assay and a thermal shift with 100μM ABL127 is detected. Using 25 or 50μM 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 体内研究 No significant decrease in tumor burden can be assessed in these pilot studies. Gel-based profiles indicate that brain PME1 is inactivated by ABL127, but overlapping serine hydrolase activities preclude a confident assessment of the extent of inactivation   推荐实验方法(仅供参考) Kinase Assay Human PME-1 protein lacking the last three amino acids (PME-1des3) is purified from Sf9 cells. The assay is completed by first conducting a 10 min pre-incubation of 1μM PME-1des3 with 100μM ABL127, 100μM AMZ-30, 100μM EHT, or vehicle (0.05 % DMSO) in the presence of SYBR Orange (1:1000, v/v) at 37°C in 1× NEB buffer 2 (50mM NaCl, 10mM Tris-HCl, 10mM MgCl2, 1mM DTT, pH 7.9 at 25 °C); a thermal gradient is performed increasing temperature by 2°C per minute increments from 37 to 95°C, and fluorescence (492 to 610nM) is acquired on a thermal cycler     Cell Assay Cells are subjected to 5 μg/mL puromycin selection for 10 to 14 days and are clonally expanded. Validated clones are incubated with media and compounds (including ABL127) for the indicated times for phenotypic assays     Animal Administration ECC-1 cells are subcutaneously inoculated into the flanks of female SCID mice and are allowed to grow until tumors reached ~400mM3 . A single intratumoral dose of ABL127 diluted in 10% DMSO/PBS is administered. The highest concentration tested is 5 mg/kg of ABL127 due to poor solubility of the compound
保存条件：-20℃

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