2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. MTHFD1/2-IN-1

MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models.

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MTHFD1/2-IN-1

MTHFD1/2-IN-1 Chemical Structure

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MTHFD1/2-IN-1 Related Antibodies

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Description

MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models[1].

In Vitro

MTHFD1/2-IN-1 (compound 34) potently inhibits the proliferation of human acute myeloid leukemia (AML) cell lines MOLM-13 (IC50=0.25 μM) and THP-1 (IC50=0.06 μM), and exhibits only moderate activity against K562, NALM-6 and MOLT-4 cells[1].
MTHFD1/2-IN-1 (0.1-10 μM; 1 h+15 min) directly interacts with human MTHFD1 and MTHFD2 proteins, which is confirmed by its dose-dependent protective effect against proteolytic degradation[1].

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

MTHFD1/2-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human AML cell lines MOLM-13, THP-1; human CML cell line K562; human ALL cell lines NALM-6, MOLT-4
Concentration: Serial dilutions
Incubation Time: 72 h
Result: Inhibited proliferation of MOLM-13 cells with an IC50 of 0.25 μM.
Inhibited proliferation of THP-1 cells with an IC50 of 0.06 μM.
Inhibited proliferation of K562 cells with an IC50 of 0.40 μM.
Inhibited proliferation of NALM-6 cells with an IC50 of 1.26 μM.
Inhibited proliferation of MOLT-4 cells with an IC50 of 1.78 μM.
In Vivo

MTHFD1/2-IN-1 (compound 34) (100-300 mg/kg; p.o.; once daily) induces dose-dependent tumor growth inhibition in an AML xenograft model, with minimal toxicity[1].

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

Animal Model: BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft model)[1]
Dosage: 100 mg/kg; 300 mg/kg
Administration: p.o.; once daily
Result: Induced tumor growth inhibition at 100 mg/kg.
Induced 79% tumor growth inhibition (TGI) at 300 mg/kg.
Maintained stable body weight across treatment period, indicating no significant treatment-related toxicity.
Molecular Weight

651.70

Formula

C30H36F3N5O6S
SMILES

CC1=C(C=CC(C2=C3CN(CC2)C(C4=CC(OC(F)(F)F)=C(C=C4)NS(N(C)CC)(=O)=O)=O)=C1OC3=O)N5C[C@@H](N(CC5)C)C
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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MTHFD1/2-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:

MTHFD1/2-IN-1Methylenetetrahydrofolate Dehydrogenase (MTHFD)nucleotide biosynthesismouse liver microsomesone-carbon metabolismacute myeloid leukemiaMTHFD2Caco-2MTHFD1human liver microsomeschronic myeloid leukemiaredox homeostasisInhibitorinhibitorinhibit

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