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| 品牌 | absin | CAS | 1404456-53-6 |
|---|---|---|---|
| 分子式 | C23H29ClN4O2S | 纯度 | 98% |
| 分子量 | 461.02 | 货号 | abs47028296 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is an orally active, allosteric Wip1 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
GSK2830371 1404456-53-6
| 产品描述 | |
| 描述 | GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 外观 | white to beige powder |
| 可溶性/溶解性 | DMSO:92 mg/mL (199.55 mM) |
| 生物活性 | |
| 靶点 | Wip1 phosphatase |
| In vitro(体外研究) | In the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increases the phosphorylation of multiple Wip1 substrates, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows selective antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Furthermore, co-treatment of doxorubicin and GSK2830371 results in a synergistic antiproliferative effect in DOHH2 and MX-1 tumor cells. |
| In vivo(体内研究) | In vivo, GSK2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreases Wip1 protein concentrations in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibits the growth of DOHH2 tumor xenografts via inhibition of Wip1. |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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