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 (130):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17383R
    Levomefolate calcium (Standard)
    		Chemical
    Levomefolate (calcium) (Standard) is the analytical standard of Levomefolate (calcium). This product is intended for research and analytical applications. Levomefolate (calcium) is an orally active, BBB-penetrable and active form of folic acid. Levomefolate (calcium) can be used as a food supplement for folic acid and in the research of neural tube defect diseases.
    Levomefolate calcium (Standard)
  • HY-122378
    Diopterin
    Diopterin is a folic acid analog that is used in leukemia research.
    Diopterin
  • HY-B1902S
    Diaveridine-d6
    Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. 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.
    Diaveridine-d<sub>6</sub>
  • HY-B0806R
    Proguanil (Standard)
    Proguanil (Standard) is the analytical standard of Proguanil. This product is intended for research and analytical applications. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil (Standard)
  • HY-105934A
    Ketotrexate sodium
    Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases.
    Ketotrexate sodium
  • 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-13664R
    Folinic acid calcium (Standard)
    		Chemical
    Folinic acid (calcium) (Standard) is the analytical standard of Folinic acid (calcium). This product is intended for research and analytical applications. 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.
    Folinic acid calcium (Standard)
  • HY-124350
    10-Formylfolic acid
    		Inhibitor
    10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid
  • 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-103396R
    Trimetrexate glucuronate (Standard)
    		Antagonist
    Trimetrexate (glucuronate) (Standard) is the analytical standard of Trimetrexate (glucuronate). This product is intended for research and analytical applications. Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.
    Trimetrexate glucuronate (Standard)
  • HY-126878
    11-Oxahomoaminopterin
    		Chemical
    11-Oxahomoaminopterin shows antifolate activity and inhibits Lactobacillus casei DHFFZ with antimicrobial and antitumor activities.
    11-Oxahomoaminopterin
  • HY-122259
    AMPte-Glu-γ-Glu
    		Inhibitor
    AMPte-Glu-γ-Glu is a substrate for folylpoly-γ-glutamate synthetase (FPGS). AMPte-Glu-γ-Glu exhibits cytotoxicity against chinese hamster ovaries cells, with IC50s of 20, 350 and 3 nM, for Pro3, R2, and 43-10, respectively.
    AMPte-Glu-γ-Glu
  • HY-13781R
    Pemetrexed disodium hemipenta hydrate (Standard)
    Pemetrexed (disodium hemipenta hydrate) (Standard) is the analytical standard of Pemetrexed (disodium hemipenta hydrate). This product is intended for research and analytical applications. 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.
    Pemetrexed disodium hemipenta hydrate (Standard)
  • HY-126830
    Antifolate C2
    Antifolate C2 is an anti-folate compound that has inhibitory effects on the proliferation of non-squamous non-small cell lung cancer (NS-NSCLC). Antifolate C2 achieves tumor selectivity by targeting proton-coupled folate transporter (PCFT), which is more selective to PCFT than the commonly used anti-folate drug Pemetrexed (HY-10820). Antifolate C2 blocks the biosynthesis of deoxypurine nucleotides by inhibiting glycinamide ribonucleotide formyltransferase (GARFTase), ultimately inhibiting the proliferation of tumor cells. Antifolate C2 can be used in studies of NS-NSCLC, especially in patients who do not respond well to Pemetrexed.
    Antifolate C2
  • HY-126119
    5,10-Dideazafolic acid
    5,10-Dideazafolic acid is a 5,10-dideaza-5,6,7,8-tetrahydrofola analogue, which exhibits some inhibitory activity against glycine amide ribonucleotide formyltransferase (GARFT) (Ki=13 μM).
    5,10-Dideazafolic acid
  • HY-13667R
    Levoleucovorin Calcium (Standard)
    		Chemical
    Levoleucovorin (Calcium) (Standard) is the analytical standard of Levoleucovorin (Calcium). This product is intended for research and analytical applications. Levoleucovorin Calcium (Calcium levofolinate), a levo isoform of Leucovorin Calcium (HY-13664), possesses antineoplastic effects. Levoleucovorin Calcium is also an augmentor of 5-fluorouracil (HY-90006) cytotoxicity against cancer.
    Levoleucovorin Calcium (Standard)
  • HY-118251
    PD130883
    PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
    PD130883
  • HY-18062R
    Pyrimethamine (Standard)
    Pyrimethamine (Standard) is the analytical standard of Pyrimethamine. This product is intended for research and analytical applications. Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate.
    Pyrimethamine (Standard)
  • HY-B0806AS
    Proguanil-d4 hydrochloride
    Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil-d<sub>4</sub> hydrochloride
  • 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)