GSK2830371

The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cdelta, 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.Formal Name: 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide. CAS Number: 1404456-53-6. Molecular Formula: C23H29ClN4O2S. Formula Weight: 461.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml, DMSO: 25 mg/ml, Ethanol: 25 mg/ml. lambdamax: 229, 255 nm. SMILES: ClC1=CC(NCC2=CC=C(C(N[C@H](C(NC3CC3)=O)CC4CCCC4)=O)S2)=C(C)N=C1. InChi Code: InChI=1S/C23H29ClN4O2S/c1-14-19(11-16(24)12-25-14)26-13-18-8-9-21(31-18)23(30)28-20(10-15-4-2-3-5-15)22(29)27-17-6-7-17/h8-9,11-12,15,17,20,26H,2-7,10,13H2,1H3,(H,27,29)(H,28,30)/t20-/m0/s1. InChi Key: IVDUVEGCMXCMSO-FQEVSTJZSA-N.