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Beschreibung

A highly cell-permeable and water soluble analog of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) 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 µ,M in in vitro kinase assay, 526 nM, 730 nM and >10 µ,M in LNCaP cells for Akt1, Akt2 and Akt3, respectively) with ~ 80-fold greater selectivity over PKA, PKC and SGK (IC50 >50 µ,M). One of its potent regioisomers (C7-substituted) is shown to enhance induced caspase-3 activity in several tumor cells., A highly cell-permeable and water soluble analog of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) 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 µ,M in in vitro kinase assay, 526 nM, 730 nM and >10 µ,M in LNCaP cells for Akt1, Akt2 and Akt3, respectively) with ~ 80-fold greater selectivity over PKA, PKC and SGK (IC50 >50 µ,M). One of its potent regioisomers (C7-substituted) is shown to enhance induced caspase-3 activity in several tumor cells.