The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer. GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM). It displays selectivity for Wip1 over 21 other phosphatases. GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53. This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.
