PROTAC HIF-1α degrader-1
Based on 1 Customer Validation
PROTAC HIF-1α degrader-1 is a potent HIF-1α PROTAC degrader. PROTAC HIF-1α degrader-1 induces ubiquitination and degradation of HIF-1α protein under hypoxic conditions. PROTAC HIF-1α degrader-1 induces Apoptosis. PROTAC HIF-1α degrader-1 can be used for the research of breast cancer and hepatocellular carcinoma.
(Pink: HIF-1α ligand (HY-111387); Blue: VHL ligand (HY-112078); Black: linker (HY-W013731)).
For research use only. We do not sell to patients.
- Purity: 98.02%
- Formula: C51H72N6O7S
- Molecular Weight:913.22
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Biological Activity
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VHL |
HIF-1α |
PROTAC HIF-1α degrader-1 (Compound V2) (24 h) potently inhibits the proliferation of MDA-MB-231 and HepG2 cells, with an IC50 of 7.54 μM for the former and 5.16 μM for the latter[1].
PROTAC HIF-1α degrader-1 (0.1-10 μM; 24 h) induces concentration-dependent degradation of HIF-1α protein in hypoxic MDA-MB-231 cells. At a concentration of 10 μM, the degradation effect is enhanced and no hook effect is observed[1].
PROTAC HIF-1α degrader-1 (3.25-7.5 μM; 24 h) induces concentration-dependent apoptosis in MDA-MB-231 cells, with the apoptosis rate reaching 48% at a concentration of 7.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human breast cancer cells, HepG2 human hepatocellular carcinoma cells
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Concentration:range of concentrations
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Incubation Time:24 h
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Result:Exhibited potent antiproliferative activity against MDA-MB-231 cells with an IC50 of 7.54 μM.
Exhibited potent antiproliferative activity against HepG2 cells with an IC50 of 5.16 μM.
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Cell Line:MDA-MB-231 human breast cancer cells (hypoxic conditions, 1% O2)
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Concentration:0.1-10 μM
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Incubation Time:24 h (under hypoxia)
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Result:Induced concentration-dependent degradation of HIF-1α protein under hypoxia, with increasing degradation observed across the tested concentration range up to 10 μM.
Showed no hook effect detected at concentrations up to 10 μM.
Demonstrated prominent degradation activity, consistent with its antiproliferative potency.
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Cell Line:MDA-MB-231 human breast cancer cells
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Concentration:3.25-7.5 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a concentration-dependent manner, with 14% apoptotic cells at 3.25 μM.
Induced apoptosis in a concentration-dependent manner, with 48% apoptotic cells at 7.5 μM.
Chemical Information
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Appearance Solid
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Molecular Weight 913.22
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Formula C51H72N6O7S
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Color White to off-white
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SMILES
O=C(N1CCN(CCOCCOCCN[C@@H](C(C)(C)C)C(N2[C@H](C(N[C@@H](C)C3=CC=C(C4=C(C)N=CS4)C=C3)=O)C[C@@H](O)C2)=O)CC1)COC5=CC=C(C67C[C@H](C[C@H](C7)C8)C[C@H]8C6)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (54.75 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 (protect from 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 (protect from 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (protect from 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.
Purity & Documentation
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Data Sheet (273 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)
- Korean - KR (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 (protect from 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 |
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| DMSO | 1 mM | 1.0950 mL | 5.4751 mL | 10.9503 mL | 27.3757 mL |
| 5 mM | 0.2190 mL | 1.0950 mL | 2.1901 mL | 5.4751 mL | |
| 10 mM | 0.1095 mL | 0.5475 mL | 1.0950 mL | 2.7376 mL | |
| 15 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8250 mL | |
| 20 mM | 0.0548 mL | 0.2738 mL | 0.5475 mL | 1.3688 mL | |
| 25 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0950 mL | |
| 30 mM | 0.0365 mL | 0.1825 mL | 0.3650 mL | 0.9125 mL | |
| 40 mM | 0.0274 mL | 0.1369 mL | 0.2738 mL | 0.6844 mL | |
| 50 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5475 mL |
PROTAC HIF-1α degrader-1 Related Classifications
HY-168641 Related Classifications
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