PHT-427
PHT-427 is an inhibitor of Akt and PDPK1 (Ki =2.7 μM and 5.2 μM, 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 8.6±0.8 μM 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 GSK3β 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.
| Storage | Store at -20°C |
| M.Wt | 409.61 |
| Cas No. | 1191951-57-1 |
| Formula | C20H31N3O2S2 |
| Solubility | insoluble in H2O; ≥20.5 mg/mL in DMSO; ≥51.1 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | PHT-427 is an inhibitor of Akt and PDPK1 with Ki values of 2.7 μM and 5.2 μM, respectively. | |||||
| Targets | Akt | PDK-1 | ||||
| IC50 | 2.7 μM(Ki) | 5.2 μM(Ki) | ||||
Quality Control & MSDS
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Chemical structure
