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描述 | The wild-type p53-induced phosphatase (Wip1, encoded by PPM1D), an oncogenic type 2C serine/threonine phosphatase common to multiple cancers, negatively regulates key proteins in the DNA damage–response pathway. GSK2830371 is the first orally active, allosteric inhibitor of Wip1 with an IC50 value of 6 nM. GSK2830371 potently inhibited Wip1 (2–420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC50 values of 6 nM and 13 nM, respectively. In the PPM1D-amplified MCF7 breast carcinoma cells, treatment with GSK2830371 for 24 h increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1 amplified, p53 wild type) with GSK2830371 caused concentration-dependent effects in cell growth assays. In a 7-d cell growth assay, GSK2830371 showed antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Co-treatment of DOHH2 and MX-1 tumor cells with the combination of GSK2830371 with doxorubicin, an anticancer agent shown to induce DNA damage, resulted in a synergistic antiproliferative effect. Unexpectively, treatment with GSK2830371 for 24 h also produced a rapid decrease in Wip1 protein concentrations. In a pharmacodynamic assay, orally administered GSK2830371 increased phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1 protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK2830371 inhibited the growth of DOHH2 tumor xenografts by 41% and 68%, respectively[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
Escherichia coli BL21 (DE3) pLysS cells | Function assay | Inhibition of His-tagged PPM1D (1 to 420 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) pLysS cells using Ac-VEPPLS(P)QETFSDLW-NH2 substrate, IC50=0.0863 μM | 26358280 | ||
MCF7 cells | Function assay | 24 h | Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs, IC50=9.5 μM | 26358280 |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.85mL 2.17mL 1.08mL |
21.69mL 4.34mL 2.17mL |
CAS号 | 1404456-53-6 |
分子式 | C23H29ClN4O2S |
分子量 | 461.02 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(108.46 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
2% DMSO+30% PEG 300+5% Tween 80+dd water 10 mg/mL |