PHT-427 is a a pleckstrin homology domain inhibitor with dual Akt and PKB Kinase (PDPK1) inhibitory activity(Ki values: Akt = 2.7 μM and PKB Kinase (PDPK1) = 5.2 μM). PHT-427 significantly reduces phosphorylation of phospho-Ser241-PKB Kinase (PDPK1) and phospho-Thr308-Akt in PC-3 prostate cancer cells which shows that PHT-427 could inhibit both Akt and PKB Kinase (PDPK1). PHT-427 also inhibits translocation of the Akt and PKB Kinase (PDPK1) PH domains in plasma membrane. PHT-427 induces apoptosis and inhibits Akt phosphorylation (IC50 = 6.3 μM), mainly on Akt Ser473 residue and less strongly on the Akt Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells (IC50 = 65 μM).
Soluble in DMSO (82 mg/ml), water (< 1 mg/ml), and ethanol (60 mg/ml).
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