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Antifolate

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<div class="colum_1 clearer"><p>Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but Raltitrexed is an inhibitor of thymidylate synthase, and Pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.</p></div>

Products Related to Antifolate(33)

  • GC10137 structure
    GC10137Trimethoprim
    CAS: 738-70-5
    Purity: >99.50%

    Trimethoprim is a bacteriostatic antibiotic inhibiting dihydrofolate reductase (DHFR) enzyme activity.

  • GC10405 structure
    GC10405Methotrexate
    CAS: 59-05-2
    Purity: >98.00%

    Methotrexate is an antifolate antimetabolite that effectively inhibits the activity of dihydrofolate reductase (DHFR), with an IC 50 of approximately 7nM.

  • GC11558 structure
    GC11558Levomefolate calcium
    CAS: 151533-22-1
    Purity: >98%

    A biologically active form of folic acid

  • GC11610 structure
    GC11610Pemetrexed
    CAS: 150399-23-8
    Purity: >99.00%

    Pemetrexed (also known as pemetrexed disodium) is a novel antifolate antimetabolite targeting multiple enzymes involved in both pyrimidine and purine synthesis.

  • GC12919 structure
    GC12919Pralatrexate
    CAS: 146464-95-1
    Purity: >98.00%

    A dihydrofolate reductase inhibitor

  • GC14331 structure
    GC14331Folinic acid
    CAS: 58-05-9
    Purity: >99.50%

    Folinic acid (FA) is an ubiquitous member of biological folate pools, usually comprising 10-20% of total cellular folates.

  • GC15306 structure
    GC15306Calcium N5-methyltetrahydrofolate
    CAS: 26560-38-3
    Purity: >98%

    Calcium salt of levomefolic acid

  • GC16203 structure
    GC16203Leucovorin Calcium
    CAS: 6035-45-6
    Purity: >98.00%

    Leucovorin Calcium (Leucovorin calcium salt pentahydrate) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.

  • GC16680 structure
    GC16680Levoleucovorin Calcium
    CAS: 80433-71-2
    Purity: >98.00%

    Levoleucovorin Calcium (Calcium levofolinate), a levo isoform of Leucovorin Calcium, possesses antineoplastic effects. Levoleucovorin Calcium is also an augmentor of 5-fluorouracil cytotoxicity against cancer.

  • GC17694 structure
    GC17694Pemetrexed disodium hemipenta hydrate
    CAS: 357166-30-4
    Purity: >99.00%
  • GC17867 structure
    GC17867Pyrimethamine
    CAS: 58-14-0
    Purity: >99.50%

    A dihydrofolate reductase inhibitor

  • GC18404 structure
    GC18404Lometrexol
    CAS: 106400-81-1
    Purity: >97.50%

    Glycinamide ribonucleotide formyltransferase (GART) is a folate-dependent enzyme required for de novo purine synthesis.

  • GC19495 structure
    GC19495DL-Folinic Acid (calcium salt)
    CAS: 1492-18-8
    Purity: >99.00%

    DL-Folinic Acid (calcium salt) (Leucovorin calcium) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.

  • GC32343 structure
    GC32343Diaveridine (EGIS-5645)
    CAS: 5355-16-8
    Purity: >98.00%

    Diaveridine (EGIS-5645) (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

  • GC32401 structure
    GC32401EC0489
    CAS: 1096702-14-5
    Purity: >98%

    EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor. Small molecule-drug conjugate (SMDC).

  • GC33322 structure
    GC33322LY 254155
    CAS: 135503-67-2
    Purity: >98%

    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.

  • GC33373 structure
    GC33373LY309887
    CAS: 127228-54-0
    Purity: >98%

    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.

  • GC34309 structure
    GC34309Cycloguanil D6 (Chlorguanide triazine D6)
    Purity: >98%
  • GC35781 structure
    GC35781Cycloguanil D6 Nitrate
    Purity: >98%

    Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.

  • GC36486 structure
    GC36486LSN 3213128
    CAS: 1941211-99-9
    Purity: >99.50%

    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.

  • GC36589 structure
    GC36589Methotrexate metabolite
    CAS: 19741-14-1
    Purity: >98.00%

    Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate.

  • GC37938 structure
    GC37938WR99210
    CAS: 47326-86-3
    Purity: >99.50%

    WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM).

  • GC39820 structure
    GC39820Lometrexol hydrate
    CAS: 1435784-14-7
    Purity: >99.00%

    A GART inhibitor

  • GC42789 structure
    GC42789Aminopterin
    CAS: 54-62-6
    Purity: >98.00%

    Aminopterin is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase, which is a cofactor for nucleic acid synthesis.