GSK 2830371 NEW
| Price | $48 | $82 | $153 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: GSK 2830371 | CAS No.: 1404456-53-6 |
| Purity: 99.3% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | GSK 2830371 |
| 描述 | GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM. |
| 細胞實驗 | 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) |
| 激酶實驗 | 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). |
| 體外活性 | 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] |
| 體內活性 | 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] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 46.1 mg/mL (100 mM) Ethanol : 23.1 mg/mL (50 mM) |
| 關鍵字 | Inhibitor | Phosphatase | GSK-2830371 | inhibit | GSK 2830371 |
| 相關產品 | PTP1B-IN-22 | Disodium monofluorophosphate | β-Glycerophosphate disodium salt pentahydrate | MLS000544460 | Tartaric acid disodium dihydrate | Cyclosporine | Stearic acid | Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride | L-Ascorbic acid 2-phosphate magnesium | Cyclosporin A | Trimyristin | β-Glycerophosphate disodium salt hydrate |
| 相關庫 | 糖代謝化合物庫 | 經典已知活性庫 | 抑制劑庫 | NO PAINS 化合物庫 | 代謝化合物庫 | 已知活性化合物庫 | 磷酸酶抑制劑化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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