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- CAS号:
1032754-81-6
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥306.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥772.0 |
| 规格: | 5mg | 产品价格: | ¥694.0 |
| 规格: | 10mg | 产品价格: | ¥1104.0 |
| 规格: | 25mg | 产品价格: | ¥2232.0 |
| 规格: | 50mg | 产品价格: | ¥3376.0 |
| 规格: | 100mg | 产品价格: | ¥4704.0 |
Product Introduction
Bioactivity
| 名称 | GNE-477 |
| 描述 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor. |
| 激酶实验 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.98 mM), Sonication is recommended. DMSO : 6.88 mg/mL (13.63 mM), Sonication is recommended. |
| 关键字 | PI3Kα | PI3K | Phosphoinositide 3-kinase | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit | GNE-477 | GNE477 |
| 相关产品 | Creatine monohydrate | L-Proline | Musk ketone | Metformin | Quercetin | Hyaluronic acid | Methyl eugenol | L-Leucine | Dihydromyricetin | Myricetin | Isoprenaline hydrochloride | Stearamide |
| 相关库 | Inhibitor Library | Pyroptosis Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Metabolism Compound Library | Kinase Inhibitor Library | Neural Regeneration Compound Library | Anti-Diabetic Compound Library | Anti-Aging Compound Library | Hematonosis Compound Library | Immunology/Inflammation Compound Library | Anti-Prostate Cancer Compound Library |
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化合物 GNE 477【1032754-81-6】
¥306 - 4704










