VHL-IN-1
Based on 1 Customer Validation
VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 3033117-53-9
- Formula: C28H37FN4O4S
- Molecular Weight:544.68
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Storage:
-20°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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
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Immunology/Inflammation Compound Library
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HY-L012
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Anti-Cancer Compound Library
HY-L025
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Reprogramming Compound Library
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Oxygen Sensing Compound Library
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Ubiquitination Compound Library
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Glutamine Metabolism Compound Library
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Anti-Breast Cancer Compound Library
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Anti-Cancer Metabolism Compound Library
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Angiogenesis-Related Compound Library
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Transcription Factor-Targeted Library
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Anti-Liver Cancer Compound Library
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Anti-Prostate Cancer Compound Library
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E3 Ligase Ligand Library
HY-L128
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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Lactylation Compound Library
HY-L249
Biological Activity
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VHL 37 nM (Kd) |
HIF-1α |
VHL-IN-1 potently binds to the VCB complex, with a dissociation constant of 37 nM as measured by fluorescence polarization (FP)[1].
VHL-IN-1 (1.37-1000 nM) binds strongly to the VCB complex, with a dissociation constant of 25 nM measured by SPR[1].
VHL-IN-1 (50 μM; 2 h) potently stabilizes total HIF-1α and hydroxylated HIF-1α in HeLa and HEK 293 cells. At the concentration of 50 μM, its induced total HIF-1α level reaches 182-224% of that induced by VH298, while the induced HIF-1α-OH level reaches 208-263% of that induced by VH298[1].
VHL-IN-1 (50-150 μM; 16 h) potently upregulates the mRNA expression of CA9 in HeLa cells, and its effects at concentrations of 100 μM and 150 μM are significantly superior to those of VH298[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, HEK 293
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Concentration:50 μM
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Incubation Time:2 h
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Result:Stabilized total HIF-1α to 182% of reference levels in HeLa cells and 224% in HEK 293 cells at 50 μM.
Stabilized HIF-1α-OH to 263% of reference levels in HeLa cells and 208% in HEK 293 cells at 50 μM.
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Cell Line:HeLa
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Concentration:50-150 μM
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Incubation Time:16 h
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Result:Significantly upregulated CA9 mRNA levels at 50 μM.
Greatly outperformed the reference inhibitor VH298 at 100 and 150 μM, reaching relative levels ~800-900% of the DMSO control at these concentrations.
Chemical Information
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CAS No. 3033117-53-9
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Appearance Solid
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Molecular Weight 544.68
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Formula C28H37FN4O4S
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°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)
Solvent & Solubility
DMSO : 100 mg/mL (183.59 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, 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)
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 1.8359 mL | 9.1797 mL | 18.3594 mL | 45.8985 mL |
| 5 mM | 0.3672 mL | 1.8359 mL | 3.6719 mL | 9.1797 mL | |
| 10 mM | 0.1836 mL | 0.9180 mL | 1.8359 mL | 4.5899 mL | |
| 15 mM | 0.1224 mL | 0.6120 mL | 1.2240 mL | 3.0599 mL | |
| 20 mM | 0.0918 mL | 0.4590 mL | 0.9180 mL | 2.2949 mL | |
| 25 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8359 mL | |
| 30 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5300 mL | |
| 40 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1475 mL | |
| 50 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 60 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7650 mL | |
| 80 mM | 0.0229 mL | 0.1147 mL | 0.2295 mL | 0.5737 mL | |
| 100 mM | 0.0184 mL | 0.0918 mL | 0.1836 mL | 0.4590 mL |
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