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 (23):

Cat. No. Product Name Effect Purity
  • HY-14519
    Methotrexate 99.85%
    Methotrexate (Amethopterin) is an antimetabolite and antifolate agent that inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate (Amethopterin) is the disease-modifying antirheumatic drug (DMARD) of first choice for the treatment of RA in most countries worldwide. Methotrexate is an antineoplastic agent used to fight a number of different cancers, such as acute lymphoblastic leukemia and solid cancers.
  • HY-10820A
    Pemetrexed disodium 99.77%
    Pemetrexed disodium (LY231514 disodium) is a novel antifolate, the Kis of the pentaglutamate of Pemetrexed disodium (LY231514 disodium) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-10820
    Pemetrexed 99.30%
    Pemetrexed (LY231514) is a novel antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
  • HY-13664
    Folinic acid calcium Chemical 99.73%
    Folinic acid calcium (Leucovorin calcium) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
  • HY-B0510
    Trimethoprim 99.98%
    Trimethoprim is a bacteriostatic antibiotic used mainly in the prophylaxis and treatment of urinary tract infections.
  • HY-107981
    LSN 3213128
    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.
  • HY-128939
    EC0488
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
  • HY-116387
    WR99210
    WR99210 is a effective inhibitor of dihydrofolate reductase (DHFR) with an IC50 of <0.075 nM. WR99210 is effective against the most pyrimethamine-resistant Plasmodium falciparum strains.
  • HY-10446
    Pralatrexate 99.23%
    Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.
  • HY-18062
    Pyrimethamine 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 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-13667
    Levoleucovorin Calcium Chemical
    Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
  • HY-B0080
    Folinic acid calcium salt pentahydrate 99.73%
    Folinic acid calcium salt pentahydrate (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.
  • HY-17383
    Levomefolate calcium Chemical
    Levomefolate calcium is an artificial form of folate.
  • HY-12784S
    Cycloguanil D6 >98.0%
    Cycloguanil D6 is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
  • HY-17556
    Folinic acid Chemical
    Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
  • HY-114306
    EC0489 Chemical
    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-14523
    LY 254155
    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-108251
    Methotrexate metabolite
    Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.
  • HY-10818
    LY309887
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
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