Potent and selective allosteric inhibitor of Wip1 phosphatase (IC50 = 6nM). 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. Orally bioavailable.
Chemical Name: 5-[[(5-Chloro-2-methyl-3-pyridinyl)amino]methyl]-N-[(1S)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide
CAS Number: 1404456-53-6
Solubility: Soluble to 100mM in DMSO and to 50mM in ethanol
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