BAY1125976

BAY1125976产品描述：BAY1125976 is a selective allosteric Akt1/2 inhibitor; inhibits Akt1 and Akt2 activity with IC₅₀ values of 5.2 nM and 18 nM at 10 μM ATP, respectively. IC50 & Target: IC50: 5.2 nM (Akt1, at 10 μM ATP), 18 nM (Akt2, at 10 μM ATP)^[1] In Vitro: BAY 1125976 is equally potent against Akt1 (IC₅₀=5.2 nM at 10 μM ATP and 44 nM at 2 mM ATP)and Akt2(IC₅₀=18 nM at 10 μM ATP and 36 nM at 2 mM ATP) isoforms and up to 86 fold less potent against Akt3 (IC₅₀=427 nM at 10 μM ATP). It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E b


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