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GSK 2830371
Catalog No. T6521Cas No. 1404456-53-6
Alias GSK2830371
GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
GSK 2830371
Catalog No. T6521Alias GSK2830371Cas No. 1404456-53-6
GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $48 | In Stock | |
| 10 mg | $82 | In Stock | |
| 25 mg | $153 | In Stock | |
| 50 mg | $267 | In Stock | |
| 100 mg | $447 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $48 | In Stock |
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β-Glycerophosphate disodium salt pentahydrate
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β-Glycerophosphate disodium salt pentahydrate is a protein phosphatase inhibitor.
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Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride
T650862746-19-2
Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride may cause sensitization. Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride promotes apoptosis in HepG2 (IC50= 62 μM) and SK-Hep1 (IC50= 151 μM) cells and inhibits protein phosphatase 2A.
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Trimyristin
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β-Glycerophosphate disodium salt hydrate
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Purity:99.3%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM. |
| Targets&IC50 | Wip1 phosphatase:6 nM |
| In vitro | 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] |
| In vivo | 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] |
| Kinase Assay | 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). |
| Cell Research | 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) |
| Alias | GSK2830371 |
| Molecular Weight | 461.02 |
| Formula | C23H29ClN4O2S |
| Cas No. | 1404456-53-6 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 46.1 mg/mL (100 mM) Ethanol: 23.1 mg/mL (50 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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