PHT-427

Short Summary : Akt and PDPK1 inhibitor

Category : PI3K/Akt/mTOR Signaling|Akt

Purity : 0.98

CAS Number : 1191951-57-1

Formula : C20H31N3O2S2

Molecular Weight : 409.61

SMILE : CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2

Solubility : >20.5mg/mL in DMSO

Storage : Store at -20°C

Description : PHT-427 is an inhibitor of Akt and PDPK1 (Ki =2.7 M and 5.2 M, respectively).
Akt is a serine/threonine-specific protein kinase that plays a vital role in multiple cellular processes including glucose metabolism, apoptosis, cell proliferation, transcription and cell migration etc.
In BxPC-3 cells, PHT-427 showed inhibition upon Akt function with IC50 value of 8.60.8 M and for its downstream substrates. PHT-427 reduced the Akt phosphorylation on Ser473 residue and did not decrease total Akt protein level. PHT-427 also inhibited p70S6K and GSK3 in a dose-dependent manner. [1][2]
In SCID (severe combined immunodeficiency) mice of BxPC-3 pancreatic cancer xenografts, administration of PHT-427 exerted prominent antitumor activity that halted tumor growth. PHT-427 in combination with erlotinib exhibited greater than additive antitumor activity in NSC lung cancer and with paclitaxel in breast cancer. [1][2]
References:1. Meuillet EJ, Zuohe S, Lemos R et al. Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther. 2010 Mar;9(3):706-17.2. Moses SA, Ali MA, Zuohe S 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 Jun 15;69(12):5073-81.

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