MDH1/2-IN-1
Based on 1 Customer Validation
MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 μM and 1.06 μM respectively). MDH1/2-IN-1 inhibits mitochondrial respiration and the HIF-1α pathway. MDH1/2-IN-1 demonstrates significant anti-tumor potential. MDH1/2-IN-1 provides a new direction for the development of drugs targeting cancer metabolism.
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 2143473-95-2
- Formula: C25H33NO4
- Molecular Weight:411.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Biological Activity
IC50: 1.07 nM (MDH1), 1.06 nM (MDH2)[1]
MDH1/2-IN-1 (Compound 16c) (60-300 μM, 0.5 h) can effectively inhibits the activity of human recombinant MDH1 (IC50: 1.07 μM) and human recombinant MDH2 (IC50: 1.06 μM)[1].
MDH1/2-IN-1 (0.1-10 μM, 12-24 h) dose-dependent inhibition of hypoxia-induced HIF-1α accumulation in human colon cancer HCT116 cells[1].
MDH1/2-IN-1 (5-20 μM ) inhibits the expression of HIF-1α target genes, including VEGF, GLUT1, and pyruvate dehydrogenase kinase 1 (PDK1), without affecting HIF-1α mRNA levels in human colon cancer HCT116 cells [1].
MDH1/2-IN-1 (1.25-10μM) significantly reduces the oxygen consumption rate (OCR) in human colon cancer HCT116 cells, inhibits mitochondrial respiration, and thus reduces the production of APT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:12-24 h
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Result:Under hypoxic conditions, HIF-1α protein accumulation is reduced and the expression of HIF-1α target genes VEGF, GLUT1, and PDK1 is downregulated
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old female nude mice; HCT116 xenograft mouse model by subcutaneously inoculating with 5 × 106 HCT116 cells in the right flank [1]
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Dosage:20 mg/kg (10 % DMSO and 10 ％ Cremophor EL and 80 % distilled water)
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Administration:i.p.
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Result:In the HCT116 xenograft model, there was a 63.4 % tumor inhibition rate, indicating potent anti-tumor activity.
No weight loss or organ toxicity (normal liver, kidney, and heart histology), indicating a wide therapeutic window.
Chemical Information
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CAS No. 2143473-95-2
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Appearance Solid
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Molecular Weight 411.53
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Formula C25H33NO4
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Color White to off-white
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SMILES
O=C(C1=CC(NC(CCOC2=CC=C(C(C)(CC(C)(C)C)C)C=C2)=O)=CC=C1)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (243.00 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. 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. 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.
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 (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. 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 | 2.4300 mL | 12.1498 mL | 24.2996 mL | 60.7489 mL |
| 5 mM | 0.4860 mL | 2.4300 mL | 4.8599 mL | 12.1498 mL | |
| 10 mM | 0.2430 mL | 1.2150 mL | 2.4300 mL | 6.0749 mL | |
| 15 mM | 0.1620 mL | 0.8100 mL | 1.6200 mL | 4.0499 mL | |
| 20 mM | 0.1215 mL | 0.6075 mL | 1.2150 mL | 3.0374 mL | |
| 25 mM | 0.0972 mL | 0.4860 mL | 0.9720 mL | 2.4300 mL | |
| 30 mM | 0.0810 mL | 0.4050 mL | 0.8100 mL | 2.0250 mL | |
| 40 mM | 0.0607 mL | 0.3037 mL | 0.6075 mL | 1.5187 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4860 mL | 1.2150 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4050 mL | 1.0125 mL | |
| 80 mM | 0.0304 mL | 0.1519 mL | 0.3037 mL | 0.7594 mL | |
| 100 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6075 mL |
MDH1/2-IN-1 Related Classifications
HY-W613220 Related Classifications
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