| Name | PHT-427 |
| 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). |
| 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. |
| 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. |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (109.86 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.88 mM), Sonication is recommended.
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| Keywords | Protein kinase B | PKB | PHT-427 | PHT427 | PDK1 | Inhibitor | inhibit | CS0223 | CS 0223 | Apoptosis | Akt |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Ethyl linoleate | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Active Compound Library |
United States
