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-10446R
    Pralatrexate (Standard)
    Pralatrexate (Standard) is the analytical standard of Pralatrexate. This product is intended for research and analytical applications. Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Pralatrexate (Standard)
  • HY-14518R
    Aminopterin (Standard)
    		Antagonist
    Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.
    Aminopterin (Standard)
  • HY-B1902R
    Diaveridine (Standard)
    Diaveridine (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.
    Diaveridine (Standard)
  • HY-107033R
    Tetroxoprim (Standard)
    		Inhibitor
    Tetroxoprim (Standard) is the analytical standard of Tetroxoprim. This product is intended for research and analytical applications. Tetroxoprim is an antimicrobial DHFR inhibitor.
    Tetroxoprim (Standard)
  • HY-139743R
    Aditoprime (Standard)
    Aditoprime (Standard) is the analytical standard of Aditoprime. This product is intended for research and analytical applications. Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics.
    Aditoprime (Standard)
  • HY-129441R
    Metoprine (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.
    Metoprine (Standard)
  • HY-B0510S3
    Trimethoprim-13C3
    Trimethoprim-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.
    Trimethoprim-<sup>13</sup>C<sub>3</sub>
  • HY-17383A
    Levomefolate disodium
    Levomefolate disodium is an orally active, BBB-penetrable and active form of folic acid. Levomefolate disodium can be used as a food supplement for folic acid and in the research of neural tube defect diseases.
    Levomefolate disodium
  • HY-123098
    Tetrahydromethotrexate
    Tetrahydromethotrexate 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.
    Tetrahydromethotrexate
  • HY-123751
    Antifolate C1
    		Inhibitor
    Antifolate C1 (AGF 94) is a GARFTase inhibitor. Antifolate C1 inhibits de novo purine biosynthesis. Antifolate C1 inhibits cell proliferation.
    Antifolate C1