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 Chemical Structure

MDH1/2-IN-1 Chemical Structure

CAS No. : 2143473-95-2

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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MDH1/2-IN-1 Related Classifications

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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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