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

Antifolate

Antifolate

Related Products

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Antifolates agents work by antagonizing (blocking) the actions of folic acid (vitamin B9). Antifolates act specifically during DNA and RNA synthesis, exerting a cytotoxic effect during the S- phase of the cell cycle. Antifolates targeting folate metabolism played a pivotal role in drug treatment of malignant, microbial, parasitic and chronic inflammatory diseases.

Folate (folic acid) cofactors are essential for the synthesis and metabolism of amino acids, 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. Major antifolate enzyme targets and exemplary antifolates that target these enzymes include: dihydrofolate reductase (DHFR), thymidylate synthase (TS), GARFTase and AICARFTase.

Antifolate Related Products (146):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0806
    Proguanil
    		99.84%
    Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil
  • HY-13781
    Pemetrexed disodium hemipenta hydrate
    		99.78%
    Pemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant 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.
    Pemetrexed disodium hemipenta hydrate
  • HY-B0080
    Folinic acid calcium salt pentahydrate
    		98.0%
    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.
    Folinic acid calcium salt pentahydrate
  • HY-17383
    Levomefolate calcium
    		99.46%
    Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia.
    Levomefolate calcium
  • HY-129441
    Metoprine
    		99.67%
    Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
    Metoprine
  • HY-B0510S
    Trimethoprim-d9
    		99.60%
    Trimethoprim-d9 is the deuterium labeled Trimethoprim. Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.
    Trimethoprim-d<sub>9</sub>
  • HY-N0913
    Manninotriose
    		Modulator 99.97%
    Manninotriose is a natural functional trisaccharide composed of three mannose molecules. Manninotriose binds to dihydrofolate reductase via hydrogen bond formation with Arg28. Manninotriose binds to thymidylate synthase via hydrogen bond formation with Arg50. Manninotriose acts as a membrane protectant and helps improve stress tolerance. Manninotriose can be used in research related to acute lymphoblastic leukemia.
    Manninotriose
  • HY-12784A
    Cycloguanil hydrochloride
    		99.93%
    Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
    Cycloguanil hydrochloride
  • HY-107981
    LSN 3213128
    		98.36%
    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. LSN 3213128 exhibits anti-tumor activity.
    LSN 3213128
  • HY-P990941
    Rinatabart
    		99.47%
    HY-P990941 is an FOLR1-targeting IgG1κ type human antibody, the recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
    Rinatabart
  • HY-10824
    Talotrexin
    		99.27%
    Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin
  • HY-10820B
    Pemetrexed disodium heptahydrate
    		Inhibitor 99.97%
    Pemetrexed disodium heptahydrate 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.
    Pemetrexed disodium heptahydrate
  • HY-10820R
    Pemetrexed (Standard)
    Pemetrexed (Standard) is the analytical standard of Pemetrexed. This product is intended for research and analytical applications. Pemetrexed (LY231514) is an 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.
    Pemetrexed (Standard)
  • HY-108251
    Methotrexate metabolite
    		98.44%
    Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.
    Methotrexate metabolite
  • HY-14519R
    Methotrexate (Standard)
    Methotrexate (Standard) is the analytical standard of Methotrexate. This product is intended for research and analytical applications. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
    Methotrexate (Standard)
  • HY-B0510R
    Trimethoprim (Standard)
    Trimethoprim (Standard) is the analytical standard of Trimethoprim. This product is intended for research and analytical applications. Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
    Trimethoprim (Standard)
  • HY-14519S
    Methotrexate-d3
    		99.83%
    Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
    Methotrexate-d<sub>3</sub>
  • HY-17556S1
    Folinic acid-d4 calcium hydrate
    		Chemical
    Folinic acid-d4-1 (Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease Methotrexate-induced toxicity.
    Folinic acid-d<sub>4</sub> calcium hydrate
  • HY-107033
    Tetroxoprim
    		Inhibitor 99.32%
    Tetroxoprim is an antimicrobial DHFR inhibitor.
    Tetroxoprim
  • HY-10818
    LY309887
    		98.23%
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
    LY309887