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PHT-427
🥰Excellent
Catalog No. T2420Cas No. 1191951-57-1
Alias PHT 427, CS-0223
PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
PHT-427
🥰Excellent
Purity: 100%
Catalog No. T2420Alias PHT 427, CS-0223Cas No. 1191951-57-1
PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | $39 | In Stock | |
| 25 mg | $79 | In Stock | |
| 50 mg | $155 | In Stock | |
| 100 mg | $263 | In Stock | |
| 200 mg | $452 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1). |
| Targets&IC50 | PDK1:5.2 μM(Ki), Akt:2.7 μM(Ki) |
| In vitro | PHT-427 had an antiproliferative effect on Panc-1 cells (IC50: 65 μM). In PC-3 prostate cancer cells, PHT-427 (10 μM) significantly decreased p-Ser241-PDPK1 and p-Thr308-Akt, indicating that PHT-427 could inhibit Akt and PDKP1. PHT-427 also inhibited the translocation of the PH domains of Akt and PDKP1 in the plasma membrane. PHT-427 induced apoptosis and inhibited AKT phosphorylation, mainly at residue Ser473 and less at residue Thr308 (IC50: 6.3 μM), with no effect on all AKT protein expression. |
| In vivo | PHT-427 had an antiproliferative effect on Panc-1 cells (IC50: 65 μM). In PC-3 prostate cancer cells, PHT-427 (10 μM) significantly decreased p-Ser241-PDPK1 and p-Thr308-Akt, indicating that PHT-427 could inhibit Akt and PDKP1. PHT-427 also inhibited the translocation of the PH domains of Akt and PDKP1 in the plasma membrane. PHT-427 induced apoptosis and inhibited AKT phosphorylation, mainly at residue Ser473 and less at residue Thr308 (IC50: 6.3 μM), with no effect on all AKT protein expression. |
| Kinase Assay | Surface plasmon resonance (SPR) spectroscopy binding assays: All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less. |
| Alias | PHT 427, CS-0223 |
| Molecular Weight | 409.61 |
| Formula | C20H31N3O2S2 |
| Cas No. | 1191951-57-1 |
| Smiles | CCCCCCCCCCCCc1ccc(cc1)S(=O)(=O)Nc1nncs1 |
| Relative Density. | 1.162 g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (109.86 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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