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Postion:Product Catalog >Biochemical Engineering>Inhibitors>PI3K / Akt / mTOR>Akt inhibitors>PHT-427
PHT-427
  • PHT-427

PHT-427 NEW

Price $39 $79 $155
Package 10mg 25mg 50mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-17

Product Details

Product Name: PHT-427 CAS No.: 1191951-57-1
Purity: 99.77% Supply Ability: 10g
Release date: 2024/11/17

Product Introduction

Bioactivity

名稱PHT-427
描述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).
激酶實驗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.
體外活性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.
體內活性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.
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 45 mg/mL (109.86 mM)
關鍵字Inhibitor | PKB | CS 0223 | Akt | CS0223 | Apoptosis | inhibit | PHT427 | Protein kinase B | PHT-427
相關產(chǎn)品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
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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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