Akt Inhibitor XIII, Isozyme-Selective, Akti-1/2 is a highly cell-permeable and water soluble analog of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (sc-202048) that acts as a plecktrin homology (PH)-domain dependent, non-ATP competitive and an allosteric inhibitor of Akt1/2 (IC50 = 560 nM, 390 nM and 7.8 μM in an in vitro kinase assay; 526 nM, 730 nM and > 10 μM in LNCaP cells for Akt1, Akt2 and Akt3, respectively) with ~ 80-fold greater selectivity over PKA, PKC and SGK (IC50 > 50 μM). One of the compounds potent regioisomers (C7-substituted) is shown to enhance induced caspase-3 activity in several tumor cells.
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PMID: # 24762137 Coomans de Brachène, A. et al. 2014. The Biochemical journal. 460: 25-34.