Antifolate
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.
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Antifolate Inhibitors
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Antifolate Antagonists
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Antifolate Modulator
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Antifolate Chemicals
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Antifolate Controls
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Antifolate Substrate
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Antifolate Ligand
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Antifolate Related Products (145)
Related Products (145)
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Lometrexol disodium
0 ImagesSynonyms: DDATHF disodiumLometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
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DHFR-IN-3
0 ImagesDHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively.
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Methotrexate α-tert-butyl ester
0 ImagesCat. No.: HY-133887CAS No.: 79640-70-3Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.
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FRα-targeting peptide C7 TFA
0 ImagesCat. No.: HY-P10501APurity: 99.85%FRα-targeting peptide C7 TFA is a selective peptide ligand for folate receptor α (FRα) that has specific binding to FRα expressing cells and in vivo tumor targeting ability. FRα-targeting peptide C7 TFA can be used in the research of tumor diagnosis and treatment.
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Trimethoprim hydrochloride
0 ImagesTrimethoprim hydrochloride is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim hydrochloride is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
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Folinic acid (Standard)
0 ImagesFolinic acid (Standard) is the analytical standard of Folinic acid. This product is intended for research and analytical applications. Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease MTX-induced toxicity.
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Proguanil hydrochloride
0 ImagesProguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
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Methotrexate γ-Methyl Ester
0 ImagesSynonyms: Methotrexate 5-methyl ester; γ-EMTXMethotrexate γ-Methyl Ester (Methotrexate 5-methyl ester) is an impurity of the folate antagonist Methotrexate (HY-14519).
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10-Formylfolic acid
0 Images10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
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Pyrimethamine-d3
0 ImagesPyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).
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Diaveridine
0 ImagesDiaveridine (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.
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Trimetrexate glucuronate
0 ImagesSynonyms: CI-898 glucuronateTrimetrexate 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.
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Aditoprime
0 ImagesSynonyms: AditoprimAditoprime (Aditoprim) is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR, respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics.
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Trimethoprim-d3
0 ImagesTrimethoprim-d3is 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.
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Levomefolate calcium (Standard)
0 ImagesLevomefolate calcium (Standard) is the analytical standard of Levomefolate calcium. This product is intended for research and analytical applications. 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.
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Mirvetuximab (powder)
0 ImagesSynonyms: M9346A (powder)Mirvetuximab (M9346A) (powder) is an anti-FOLR1 (folate receptor 1) monoclonal antibody. Mirvetuximab (powder) is the antibody moiety of folate receptor alpha (FRα)-targeting ADC (Mirvetuximab soravtansine). Mirvetuximab soravtansine can be used in ovarian and other FRα-positive cancer research.
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Fanotaprim
0 ImagesSynonyms: VYR-006Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis.
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Glutamate carboxypeptidase
0 ImagesGlutamate carboxypeptidase is an endo/exopeptidase targeting folate and antifolate agents. Glutamate carboxypeptidase regulates intracellular folate homeostasis by hydrolyzing γ-polyglutamate chains. Glutamate carboxypeptidase is promising for research of antifolate agents and cancers.
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Nolatrexed
0 ImagesCat. No.: HY-13714CAS No.: 147149-76-6Synonyms: AG 337 free baseNolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.
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Cycloguanil
0 ImagesCycloguanil (Chlorguanide triazine) is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil 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 also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
