化合物GSK2830371 T6521

Product Introduction
Bioactivity


英文名: GSK 2830371

描述: GSK 2830371 是 Wip1磷酸酶 (Wip1 phosphatase)选择性抑制剂，IC50=6 nM。

细胞实验: Cells are seeded into 96 well plates at 200–400 cells per well and treated with a compound dilution series on day 1. After 7 d, The CellTiter-Glo cell viability assay is used to determine effects on cell growth. Luminescent signal is detected on an EnVision 2104.(Only for Reference)

激酶实验: In vitro phosphatase assays: The primary in vitro Wip1 enzymatic assay measures fluorescence generated by Wip-1 (2–420) hydrolysis of fluorescein diphosphate (FDP). 50 μM FDP substrate with compound or DMSO is added at room temperature before addition of 10 nM Wip1 in assay buffer (50 mM TRIS, pH 7.5, 30 mM MgCl2, 0.8 mM CHAPS, 0.05 mg/ml BSA). Fluorescent signal is detected on a Spectramax microplate reader (485/530 nm).

体外活性: 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. [1]

体内活性: 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. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 46.1 mg/mL (100 mM)
Ethanol : 23.1 mg/mL (50 mM)


关键字: Inhibitor | Phosphatase | GSK-2830371 | inhibit | GSK 2830371

相关产品: Ascomycin | Etidronic acid | Anticancer agent 144 | Tetramisole hydrochloride | 2-Bromo-4'-hydroxyacetophenone | CPDA | h-NTPDase-IN-5 | Salubrinal | SHIP2-IN-1 | Sodium stibogluconate

相关库: Glycometabolism Compound Library | Bioactive Compounds Library Max | Phosphatase Inhibitor Library | Inhibitor Library | Metabolism Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途