1. Cell Cycle/DNA Damage
  2. 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 (16):

Cat. No. Product Name Effect Purity
  • HY-14519
    Methotrexate Antagonist 99.69%
    Methotrexate is a traditional folate antagonist, with median IC50 of 78 nM for a 120 h drug exposure in a panel of six pediatric leukemia and lymphoma cell lines using the sulforhodamine B assay.
  • HY-10820A
    Pemetrexed disodium Antagonist 99.04%
    Pemetrexed disodium 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-10446
    Pralatrexate Inhibitor 98.64%
    Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.
  • HY-14781
    Levomefolic acid Agonist >98.0%
    Levomefolic acid (5-MTHF) is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.
  • HY-13664
    Folinic acid Calcium Agonist 99.97%
    Leucovorin Calcium is a reduced folic acid.
  • HY-18062
    Pyrimethamine Antagonist 99.93%
    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-B0080
    Folinic acid calcium salt pentahydrate Antagonist 99.39%
    Folinic Acid is a reduced folic acid, which is used in combination with other chemotherapy drugs.
  • HY-13781
    Pemetrexed disodium hemipenta hydrate Inhibitor 99.78%
    Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
  • 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-B0510
    Trimethoprim Inhibitor
    Trimethoprim is a bacteriostatic antibiotic used mainly in the prophylaxis and treatment of urinary tract infections.
  • HY-12784S
    Cycloguanil D6 Antagonist
    Cycloguanil D6 is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
  • HY-12784S1
    Cycloguanil D6 Nitrate Antagonist
    Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
  • HY-10820
    Pemetrexed Inhibitor
    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-13667
    Levoleucovorin Calcium Agonist
    Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
  • 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.