Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK 2830371 是 Wip1磷酸酶 (Wip1 phosphatase)选择性抑制剂,IC50=6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 195 | 现货 | ||
5 mg | ¥ 479 | 现货 | ||
10 mg | ¥ 788 | 现货 | ||
25 mg | ¥ 1,480 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 3,930 | 现货 | ||
200 mg | ¥ 5,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 593 | 现货 |
产品描述 | GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM. |
靶点活性 | Wip1 phosphatase:6 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] |
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). |
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) |
别名 | GSK2830371 |
分子量 | 461.02 |
分子式 | C23H29ClN4O2S |
CAS No. | 1404456-53-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 46.1 mg/mL (100 mM)
Ethanol: 23.1 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.1691 mL | 10.8455 mL | 21.691 mL | 54.2276 mL |
5 mM | 0.4338 mL | 2.1691 mL | 4.3382 mL | 10.8455 mL | |
10 mM | 0.2169 mL | 1.0846 mL | 2.1691 mL | 5.4228 mL | |
20 mM | 0.1085 mL | 0.5423 mL | 1.0846 mL | 2.7114 mL | |
50 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0846 mL | |
DMSO | 100 mM | 0.0217 mL | 0.1085 mL | 0.2169 mL | 0.5423 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK 2830371 1404456-53-6 Metabolism Phosphatase Inhibitor GSK-2830371 GSK2830371 inhibit inhibitor