| 应用 |
A pleckstrin homology domain inhibitor to Akt and PKB Kinase (PDPK1). |
| 产品介绍 |
PHT-427是作用于Akt和PDPK1的双重抑制剂，Akt和PDPK1的PH结构域具有高度亲和力，Ki分别为2.7 μM和5.2 μM。 |
| 备注 |
PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively. |
| 生化机理 |
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). |
| 别名 |
PHT 427; 4-十二烷基-N-1,3,4-噻二唑-2-基苯磺酰胺;PHT 427;PHT427;4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide |
