1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Antifolate

Antifolate

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.

Antifolate Related Products (19):

Cat. No. Product Name Effect Purity
  • HY-14519
    Methotrexate Antagonist 99.75%
    Methotrexate is a folate antagonist, with median IC50 of 78 nM in in vitro assay.
  • HY-10820A
    Pemetrexed disodium Inhibitor 99.77%
    Pemetrexed disodium is a novel antifolate that inhibits the folatedependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase with Kis of 1.3, 7.2, and 65 nM, respectively.
  • HY-13664
    Folinic acid Calcium Agonist 99.73%
    Leucovorin Calcium is a reduced folic acid.
  • HY-10820
    Pemetrexed Inhibitor 99.30%
    Pemetrexed is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-B0510
    Trimethoprim Inhibitor 99.98%
    Trimethoprim is a bacteriostatic antibiotic used mainly in the prophylaxis and treatment of urinary tract infections.
  • HY-114306
    EC0489 Modulator
    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).
  • HY-10446
    Pralatrexate Inhibitor 99.23%
    Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.
  • HY-18062
    Pyrimethamine Antagonist 99.90%
    Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).
  • HY-13781
    Pemetrexed disodium hemipenta hydrate Inhibitor 99.78%
    Pemetrexed disodium hemipenta hydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-B0080
    Folinic acid calcium salt pentahydrate Antagonist 99.73%
    Folinic acid (calcium salt pentahydrate) is a reduced folic acid, which is used in combination with other chemotherapy drugs.
  • HY-13667
    Levoleucovorin Calcium Agonist
    Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
  • HY-12784S
    Cycloguanil D6 Antagonist >98.0%
    Cycloguanil D6 is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
  • HY-17383
    Levomefolate calcium Agonist
    Levomefolate is an artificial form of folate.
  • HY-17556
    Folinic acid Agonist
    Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.
  • HY-14523
    LY 254155 Inhibitor
    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
  • HY-12784S1
    Cycloguanil D6 Nitrate Antagonist
    Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
  • HY-B1902
    Diaveridine Inhibitor 98.48%
    Diaveridine (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.
  • HY-10818
    LY309887 Inhibitor
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
  • HY-17557
    Calcium N5-methyltetrahydrofolate Agonist
    Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
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