FPA-124 is a cell-permeable inhibitor of Akt (IC50 = 100 nM), binding to the PH and kinase domains. It inhibits cell proliferation in Colo357, BxPC3, BT20, and PC3 cancer cell lines with IC50 values ranging from 7-55 nM. FPA-124 inhibited tumor growth in mice with negligible toxicity.
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Derivatives of Chromen-4-one in Human Cancer Cells” J. Med. Chem., 2006, 49, 3800-3808.
2) Biscetti, F., G. Straface, et al. (2009). “Pioglitazone enhances collateral blood flow in ischemic hindlimb of diabetic mice through an Akt-dependent VEGF-mediated mechanism, regardless of PPARgamma stimulation.” Cardiovasc Diabetol 8: 49.
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