GSK2830371

The serine/threonine phosphatase Wip1 plays an important role in tumor development. Despite its aberrant activity characterizing different forms of cancer, selective inhibitors are still lacking. GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with an IC50 of 6 nM. It binds to a flap subdomain that regulates Wip1's enzymatic activity and substrate recognition. Due to lack of this domain in other phosphatases, its binding to GSK2830371 results in a selective and potent inhibition of Wip1. When tested in animal models suffering from a blood cancer (lymphoma), GSK2830371effectively blocked the tumoral growth.

Store at 0° C (short term), -20° C (long term), desiccated

HPLC-MS, ¹HNMR, Chiral HPLC and Quantitative Elemental Analysis

A.G.Gilmartin, et al, Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction, Nature Chemical Biology 10, 181-187 (2014)