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 (150)
Related Products (150)
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Diaveridine (Standard)
0 ImagesDiaveridine (Standard) is the analytical standard of Diaveridine. This product is intended for research and analytical applications. 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.
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Tetroxoprim (Standard)
0 ImagesSynonyms: HE 781 (Standard)Tetroxoprim (Standard) is the analytical standard of Tetroxoprim. This product is intended for research and analytical applications. Tetroxoprim is an antimicrobial DHFR inhibitor.
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Aditoprime (Standard)
0 ImagesCat. No.: HY-139743RCAS No.: 56066-63-8Synonyms: Aditoprim (Standard)Aditoprime (Standard) 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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Metoprine (Standard)
0 ImagesSynonyms: BW 197U (Standard)Metoprine (Standard) is the analytical standard of Metoprine. This product is intended for research and analytical applications. 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.
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Trimethoprim-13C3
0 ImagesCat. No.: HY-B0510S3CAS No.: 1189970-95-3Trimethoprim-13C3 is the deuterium labeled Trimethoprim (HY-B0510). 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.
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Trimetrexate (Standard)
0 ImagesCat. No.: HY-10373RCAS No.: 52128-35-5Synonyms: CI-898 (Standard)Trimetrexate (Standard) is the analytical standard of Trimetrexate (HY-10373). This product is intended for research and analytical applications. Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
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LY309887 (Standard)
0 ImagesCat. No.: HY-10818RCAS No.: 127228-54-0
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Levomefolate disodium
0 ImagesCat. No.: HY-17383ACAS No.: 1423663-76-6Levomefolate disodium is a synthetic disodium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate disodium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate disodium does not significantly increase folate concentrations in breast milk. Levomefolate disodium can be used for the research of neural tube defects and megaloblastic anemia.
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Tetrahydromethotrexate
0 ImagesTetrahydromethotrexate is a more potent folate antagonist than Methotrexate (HY-14519) in studies against certain bacteria (Streptococcus faecalis, Pediococcus erevisiae) and in animal models. Tetrahydromethotrexate is used in the research of cancer and autoimmune diseases.
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Antifolate C1
0 ImagesCat. No.: HY-123751CAS No.: 136784-51-5Synonyms: AGF 94Antifolate C1 (AGF 94) is a GARFTase inhibitor. Antifolate C1 inhibits de novo purine biosynthesis. Antifolate C1 inhibits cell proliferation.
