2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. MTHFD2-IN-7

MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research.

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MTHFD2-IN-7

MTHFD2-IN-7 Chemical Structure

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MTHFD2-IN-7 Related Antibodies

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Description

MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research[1].

In Vitro

MTHFD2-IN-7 (compound 31) inhibits the proliferation of human leukemia cell lines[1].
MTHFD2-IN-7 (0.1-10 μM; 1 h+15 min) binds to and protects purified human MTHFD2 and MTHFD1 from pronase degradation in a dose-dependent manner, with such effects observed at concentrations of 0.1, 1.0 and 10 μM, which confirms its direct binding to the targets[1].

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

MTHFD2-IN-7 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human leukemia cell lines: MOLM-13, THP-1, K562, NALM-6 and MOLT-4
Concentration: IC50
Incubation Time: 72 h
Result: Inhibited the proliferation of human leukemia cell lines, with IC50 values of 0.72 μM (MOLM-13), 0.25 μM (THP-1), 0.84 μM (K562), 2.45 μM (NALM-6) and 4.75 μM (MOLT-4).
In Vivo

MTHFD2-IN-7 (compound 31) (100-300 mg/kg; p.o.; once daily) induces dose-dependent tumor growth inhibition in MOLM-13 AML xenografts, with no significant toxicity[1].

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

Animal Model: BALB/c nude mice with Acute myeloid leukemia (female, 6−8 weeks old)[1]
Dosage: 100 mg/kg; 300 mg/kg
Administration: p.o.; once daily
Result: Achieved 37% tumor growth inhibition at 100 mg/kg.
Achieved 67% tumor growth inhibition at 300 mg/kg.
Showed no significant body weight loss, indicating well tolerated treatment.
Molecular Weight

623.64

Formula

C28H32F3N5O6S
SMILES

CC1=C(C=CC(C2=C3CN(CC2)C(C4=CC(OC(F)(F)F)=C(C=C4)NS(NC)(=O)=O)=O)=C1OC3=O)N5C[C@@H](N(CC5)C)C
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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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MTHFD2-IN-7 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:

MTHFD2-IN-7Methylenetetrahydrofolate Dehydrogenase (MTHFD)MTHFD2MOLM-13K562Caco-2acute myeloid leukemiacancer cell proliferationNAD+NALM-6THP-1MTHFD1Inhibitorinhibitorinhibit

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