PHT-427 NEW
Price | $39 | $79 | $155 |
Package | 10mg | 25mg | 50mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: PHT-427 | CAS No.: 1191951-57-1 |
Purity: 99.77% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
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 | 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) |
Keywords | Inhibitor | PKB | CS 0223 | Akt | CS0223 | Apoptosis | inhibit | PHT427 | Protein kinase B | PHT-427 |
Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | 2,3-Butanediol |
Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Anti-Cancer Active Compound Library | Oxidation-Reduction Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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