2. Metabolic Enzyme/Protease
  3. Malate Dehydrogenase (MDH) HIF/HIF Prolyl-Hydroxylase Mitochondrial Metabolism
  4. MDH1/2-IN-1

MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 nM and 1.06 nM 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.

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MDH1/2-IN-1

MDH1/2-IN-1 Chemical Structure

CAS No. : 2143473-95-2

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Based on 1 publication(s) in Google Scholar

MDH1/2-IN-1 Related Antibodies

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Description

MDH1/2-IN-1 is a MDH1/2 inhibitor (IC50: 1.07 nM and 1.06 nM 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[1].

IC50 & Target

IC50: 1.07 nM (MDH1), 1.06 nM (MDH2)[1]
In Vitro

MDH1/2-IN-1 (Compound 16c) (60-300 μM, 0.5 h) can effectively inhibits the activity of human recombinant MDH1 (IC50: 1.07 nM) and human recombinant MDH2 (IC50: 1.06 nM)[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.

MDH1/2-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 12-24 h
Result: Under hypoxic conditions, HIF-1α protein accumulation is reduced and the expression of HIF-1α target genes VEGF, GLUT1, and PDK1 is downregulated
In Vivo

MDH1/2-IN-1 (Compound 16c) (20 mg/kg, i.p. once a day for 14 consecutive days) reduces tumor growth by 63.4 % without significant toxicity, in the HCT116 colon cancer xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 20 mg/kg (10 % DMSO and 10 ％ Cremophor EL and 80 % distilled water)
Administration: i.p.
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.
Molecular Weight

411.53

Formula

C25H33NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(NC(CCOC2=CC=C(C(C)(CC(C)(C)C)C)C=C2)=O)=CC=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4300 mL 12.1498 mL 24.2996 mL
5 mM 0.4860 mL 2.4300 mL 4.8599 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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MDH1/2-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MDH1/2-IN-12143473-95-2Malate Dehydrogenase (MDH)HIF/HIF Prolyl-HydroxylaseMitochondrial MetabolismMalate DehydrogenaseHypoxia-inducible factorsHIFsHIF-PHMDH1/2 inhibitormitochondrial respirationHIF-1HCT116 cell mouse modelcolorectal cancerInhibitorinhibitorinhibit

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