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].
Molecular Weight:
623.64
Formula:
C28H32F3N5O6S
Target:
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
Application Notes:
MCE Product type: Reference compound
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