Potent and selective allosteric inhibitor of Wip1 phosphatase (IC50 = 6 nM). Exhibits selectivity for Wip1 over 21 other phosphatases. Increases phosphorylation of Wip1 substrates, including p53, Chk2, H2AX and ATM. Attenuates tumor cell growth in a variety of lymphoid cell lines. Also inhibits lymphoma xenograft growth in vivo. Potentiates growth inhibitory effects of MDM2 inhibition in cancer cell lines in a p53-dependent manner. Orally bioavailable.
Sold for research purposes only under agreement from GlaxoSmithKline
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 461.02. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.17 mL||10.85 mL||21.69 mL|
|5 mM||0.43 mL||2.17 mL||4.34 mL|
|10 mM||0.22 mL||1.08 mL||2.17 mL|
|50 mM||0.04 mL||0.22 mL||0.43 mL|
References are publications that support the biological activity of the product.
Gilmartin et al (2014) Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 10 181 PMID: 24390428
Esfandiari et al (2016) Chemical inhibition of wild-type p53-induced phosphatase 1 (WIP1/PPM1D) by GSK2830371 potentiates the sensitivity to MDM2 inhibitors in a p53-dependent manner. Mol.Cancer Ther. 15 379 PMID: 26832796
If you know of a relevant reference for GSK 2830371, please let us know.
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Keywords: GSK 2830371, GSK 2830371 supplier, GSK2830371, potent, selective, allosteric, inhibitors, inhibits, wip1, phosphatases, antitumor, orally, bioavailable, Protein, Ser/Thr, Phosphatases, 5140, Tocris Bioscience
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