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GNE-477

Catalog No. T3692   CAS 1032754-81-6
Synonyms: GNE 477

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GNE-477 Chemical Structure
GNE-477, CAS 1032754-81-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 89.00
2 mg In stock $ 118.00
5 mg In stock $ 169.00
10 mg In stock $ 288.00
25 mg In stock $ 583.00
50 mg In stock $ 836.00
100 mg In stock $ 1,160.00
1 mL * 10 mM (in DMSO) In stock $ 227.00
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Purity: 99.95%
Purity: 98.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
Targets&IC50 mTOR:21 nM(Ki app), PI3Kα:4 nM
Kinase Assay Fluorescence Polarization Based Assays for XIAP, cIAP1, and cIAP2 BIR3 Proteins: FL-AT-406 (the fluorescently tagged AT-406) is employed to develop a set of new FP assays for determination of the binding affinities of Smac mimetics to XIAP, cIAP-1, and cIAP-2 BIR3 proteins. The Kd value of FL-AT-406 to each IAP protein is determined by titration experiments using a fixed concentration of FL-AT-406 and different concentrations of the protein up to full saturation. Fluorescence polarization values are measured using an Infinite M-1000 plate reader in Microfluor 2 96-well, black, round-bottom plates. To each well, FL-AT-406 (2, 1, and 1 nM for experiments with XIAP BIR3, cIAP-1 BIR3, and cIAP-2 BIR3, respectively) and different concentrations of the protein are added to a final volume of 125 μL in the assay buffer (100 mM potassium phosphate, pH 7.5, 100 μg/mL bovine γ-globulin, 0.02% sodium azide, with 4% DMSO). Plates are mixed and incubated at room temperature for 2-3 hours with gentle shaking. The polarization values in millipolarization units (mP) are measured at an excitation wavelength of 485 nm and an emission wavelength of 530 nm. Equilibrium dissociation constants (Kd) are then calculated by fitting the sigmoidal dose-dependent FP increases as a function of protein concentrations using Graphpad Prism 5.0 software. In competitive binding experiments for XIAP3 BIR3, AT-406 is incubated with 20 nM XIAP BIR3 protein and 2 nM FL-AT-406 in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/mL bovine γ-globulin; 0.02% sodium azide). In competitive binding experiments for cIAP1 BIR3 protein, 3 nM protein and 1 nM FL-AT-406 are used. In competitive binding experiments for cIAP2 BIR3, 5 nM protein and 1 nM FL-AT-406 are used. For each competitive binding experiment, polarization values are measured after 2-3 hours of incubation using an Infinite M-1000 plate reader.The IC50 value, the inhibitor concentration at which 50% of the bound tracer is displaced, is determined from the plot using nonlinear least-squares analysis. Curve fitting is performed using the PRISM software. A Ki value for AT-406 is calculated.
Synonyms GNE 477
Molecular Weight 504.63
Formula C21H28N8O3S2
CAS No. 1032754-81-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.88 mg/mL (13.62 mM)

TargetMolReferences and Literature

1. Heffron TP, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11.

Related compound libraries

This product is contained In the following compound libraries:
Neural Regeneration Compound Library Oxidation-Reduction Compound Library Inhibitor Library Reprogramming Compound Library Glycolysis Compound Library Glycometabolism Compound Library Anti-Prostate Cancer Compound Library Pyroptosis Compound Library Anti-Liver Cancer Compound Library Anti-Breast Cancer Compound Library

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Keywords

GNE-477 1032754-81-6 PI3K/Akt/mTOR signaling PI3K mTOR Phosphoinositide 3-kinase GNE 477 Inhibitor GNE477 Mammalian target of Rapamycin inhibit inhibitor

 

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