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DHFR

Dihydrofolate reductase (DHFR) inhibitors block the enzyme that reduces dihydrofolate to tetrahydrofolate. Tetrahydrofolate carries one-carbon units for the synthesis of thymidylate, purines and several amino acids, so DHFR inhibition starves dividing cells of DNA precursors. In 1958 aminopterin and amethopterin, the compound now called methotrexate, were shown to inhibit the enzyme. Methotrexate, aminopterin and pralatrexate are classical antifolates, whereas the lipophilic trimetrexate enters cells without the folate carrier. Pemetrexed, described in 1997 as LY231514, also inhibits thymidylate synthase and glycinamide ribonucleotide formyltransferase. Proguanil, whose metabolite cycloguanil acts on the parasite enzyme, and the diaminopyrimidine diaveridine represent inhibitors of microbial DHFR.

1 Item

  • Aminopterin sodium
    Cat. No.
    A54043
    CAS No.
    58602-66-7

    Aminopterin sodium

    Synonyms: 4-Aminofolic acid sodium; APGA sodium

    Aminopterin sodium is a folic acid antagonist that primarily targets dihydrofolate reductase (DHFR). By inhibiting DHFR, it disrupts folate metabolism, leading to decreased nucleic acid synthesis. This compound is primarily utilized in the treatment of acute lymphoblastic leukemia and various cancers. Additionally, Aminopterin sodium is employed as an immunosuppressant for the management of autoimmune disorders.

    In stock View Details
    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

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