THS-044
Based on 1 Customer Validation
THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (KD = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia.
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- Reinheit: 99.37%
- CAS. Nr.: 62054-67-5
- Formel: C11H12F3N3O3
- Molecular Weight:291.23
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
THS-044 (50 μM) binds wild-type human HIF2α PAS-B protein with a 1:1 stoichiometry and a Kd value of 2 μM[1].
THS-044 (50 μM excess) stabilizes HIF2α PAS-B against trypsin-mediated proteolysis at sites distal to the R330 cleavage site and enhances the stability of its β-sheet region, elevating ²H exchange protection factors by up to 100-fold at certain positions[1].
THS-044 (100 μM excess) occupies the internal cavity of HIF2α PAS-B within the high-affinity PAS-B heterodimer with only minor protein side-chain rearrangements, and reduces the binding affinity of the wild-type HIF2α PAS-B/ARNT PAS-B heterodimer, increasing its Kd from 120 μM to 400 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 62054-67-5
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Appearance Solid
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Molecular Weight 291.23
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Formel C11H12F3N3O3
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Color Yellow to orange
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SMILES
FC(C1=CC=C(NN2CCOCC2)C([N+]([O-])=O)=C1)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (429.21 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Scheuermann TH, et al. Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc Natl Acad Sci U S A. 2009 Jan 13;106(2):450-455. [Content Brief]
[2]. Nordgren IK, et al. Targeting tumour angiogenesis with small molecule inhibitors of hypoxia inducible factor. Chem Soc Rev. 2011;40(8):4307-4317. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4337 mL | 17.1686 mL | 34.3371 mL | 85.8428 mL |
| 5 mM | 0.6867 mL | 3.4337 mL | 6.8674 mL | 17.1686 mL | |
| 10 mM | 0.3434 mL | 1.7169 mL | 3.4337 mL | 8.5843 mL | |
| 15 mM | 0.2289 mL | 1.1446 mL | 2.2891 mL | 5.7229 mL | |
| 20 mM | 0.1717 mL | 0.8584 mL | 1.7169 mL | 4.2921 mL | |
| 25 mM | 0.1373 mL | 0.6867 mL | 1.3735 mL | 3.4337 mL | |
| 30 mM | 0.1145 mL | 0.5723 mL | 1.1446 mL | 2.8614 mL | |
| 40 mM | 0.0858 mL | 0.4292 mL | 0.8584 mL | 2.1461 mL | |
| 50 mM | 0.0687 mL | 0.3434 mL | 0.6867 mL | 1.7169 mL | |
| 60 mM | 0.0572 mL | 0.2861 mL | 0.5723 mL | 1.4307 mL | |
| 80 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.0730 mL | |
| 100 mM | 0.0343 mL | 0.1717 mL | 0.3434 mL | 0.8584 mL |
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