HIF-1/2α-IN-2
Based on 1 Customer Validation
HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).
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- Pureza: 99.55%
- No. CAS: 862974-22-9
- Fòrmula: C16H11FN4O2S
- Peso molecular:342.35
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
Iron Sulfur Cluster Assembly 2 (ISCA2), HIF-1/2α[1]
HIF-1/2α-IN-2 (compound #1) (0-25 μM; 24 h) decreases HIF-2α translation instead of transcription, with a downward trend in VEGFA and POU5F1 (HIF-2α target genes) transcription and insignificant effect on EPAS1 (HIF-2α)[1].
HIF-1/2α-IN-2 (0-100 μM, 24 h) inhibits the production of luciferase driven by the HIF-2α Iron-Responsive Element (IRE) luciferase reporter with an IC50 value of 3.9 μM, to block IRE-dependent translation of HIF-2α[1].
HIF-1/2α-IN-2 (0, 10, 50 μM) protects ISCA2 from Pronase-mediated (4 μg/mL) degradation, and (1.5 μM; 24 h) targets ISCA2 to induce iron and metals accumulation in normoxia 786-0 cells[1].
HIF-1/2α-IN-2 (0-100 μM; 24 h) results ISCA2 inhibition and promotes cell death via ferroptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normoxia 786-0 cells (20%O2) and hypoxic ACHN cells (or 1%O2 for final 24 h to induce HIF expression)
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Concentration:0, 1, 5, 10, 25 μM
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Incubation Time:24 hours
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Result:Decreased the protein level of HIF-2α, FTH1, ISCA2, and increased IRP2 protein level at high concentrations over 10 μM in normoxia 786-0 cells.
Dcreased the HIF-2α and FTH1 levels at 1 μM in hypoxic ACHN cells.
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Cell Line:Normoxia 786-0 cells
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Concentration:0-100 μM
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Incubation Time:24 hours
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Result:Inhibited 786-0 cells viability by inducing ferroptosis, with an IC50 value of 22.0 μM.
Chemical Information
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No. CAS 862974-22-9
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Appearance Solid
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Peso molecular 342.35
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Fòrmula C16H11FN4O2S
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Color White to off-white
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SMILES
COC1=C2N=C(NC3=NN=C(C4=CC=C(F)C=C4)O3)SC2=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 50 mg/mL (146.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9210 mL | 14.6049 mL | 29.2099 mL | 73.0247 mL |
| 5 mM | 0.5842 mL | 2.9210 mL | 5.8420 mL | 14.6049 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9210 mL | 7.3025 mL | |
| 15 mM | 0.1947 mL | 0.9737 mL | 1.9473 mL | 4.8683 mL | |
| 20 mM | 0.1460 mL | 0.7302 mL | 1.4605 mL | 3.6512 mL | |
| 25 mM | 0.1168 mL | 0.5842 mL | 1.1684 mL | 2.9210 mL | |
| 30 mM | 0.0974 mL | 0.4868 mL | 0.9737 mL | 2.4342 mL | |
| 40 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8256 mL | |
| 50 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4605 mL | |
| 60 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2171 mL | |
| 80 mM | 0.0365 mL | 0.1826 mL | 0.3651 mL | 0.9128 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7302 mL |
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