GSK 2830371

Key Product Details

Product Description

GSK 2830371 is a 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.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Product Specifications for GSK 2830371

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GSK 2830371

The following data is based on the product molecular weight 461.02.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 6 publications citing the usage of this product.

• Esfandiari 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. 2016 PMID: 26832796
• Gilmartin Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction. Nat.Chem.Biol. 2014 PMID: 24390428

Product Documents for GSK 2830371