PHT-427_1191951-57-1_DataSheet_MedChemExpress

P d D Sh
Product Name:
PHT-427CAS No.:
1191951-57-1Cat. No.:
HY-12063Product Data Sheet MWt:
409.61Formula:
C20H31N3O2S2Purity :>98%
Solubility:DMSO ≥80mg/mL Water ≥
46/L Eth l 80/
L Mechanisms:
Biological Activity:
PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and
Pathways:PI3K/Akt/mTOR ; Target:Akt 4.6mg/mL Ethanol
≥80mg/mL
PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.
IC50 value: 2.7/5.2 uM (Ki, Akt/PDPK1) [1]
Target: Akt/PDPK1in vitro: PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM,which shows that PHT-427 could inhibit both Akt and PDKP1. PHT-427 also inhibits translocation of the Akt and PDKP1 PH domains in plasma membrane [1]. PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308residue without affecting total Akt protein expression PHT 427also shows References:
[1]. Meuillet EJ, et al. Molecular pharmacology and antitumor activity of PHT-427 a novel
AKT/PDPK1 pleckstrin homology domain inhibitor. Mol Cancer Ther, 2010, 9(3), 706-717.[2]Moses SA et al In vitro and in vivo activity of novel small molecule inhibitors targeting the less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows
antiproliferation in Panc-1 cells with IC50 of 65 μM [2].in vivo: PHT-427 shows great antitumor activi...
[2]. Moses SA, et al. In vitro and in vivo activity of novel small-molecule inhibitors targeting the
pleckstrin homology domain of protein kinase B/AKT. Cancer Res, 2009, 69(12), 5073-5081.Caution: Not fully tested. For research purposes only
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