We use analytics and advertising cookies, which you can accept or reject; see our privacy policy.

Current choice:

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.

3 Items

  • BION106
    Cat. No.
    A43983
    CAS No.
    3077918-44-3

    BION106

    BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC DHFR Degrader-1
    Cat. No.
    A43992
    CAS No.
    3077918-47-6

    PROTAC DHFR Degrader-1

    PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum.

    View Details

    Out of stock

    All 3 sizes
  • PROTAC eDHFR Degrader-1
    Cat. No.
    A84545
    CAS No.
    2849442-92-6

    PROTAC eDHFR Degrader-1

    PROTAC eDHFR Degrader-1 is a proteolysis-targeting chimera (PROTAC) that specifically targets eDHFR for ubiquitin-mediated degradation. This compound effectively degrades eDHFR-YFP and various protein of interest (POI), including yellow fluorescent protein (YFP) and luciferase. Its application in research can facilitate the study of protein function and dynamics through targeted protein degradation, providing insights into cellular processes and potential therapeutic pathways.

    In stock View Details
    5 mg
    $500.00
    10 mg
    $825.00
    All 4 sizes

3 Items

Added to your cart

View Cart Checkout

    Loading...