Gsk 2830371, Potent And Selective Allosteric Inhibitor Of Wip1 Phosphatase, Each

Details:

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.