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 (117):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-W654270
    Calcium N5-methyltetrahydrofolate-d3
    		Chemical
    Calcium N5-methyltetrahydrofolate-d3 is deuterium labeled Calcium N5-methyltetrahydrofolate.
    Calcium N5-methyltetrahydrofolate-d<sub>3</sub>
  • 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-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-17556R
    Folinic acid (Standard)
    		Chemical
    Folinic 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 (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity.
    Folinic acid (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-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, blood-brain barrier-crossing form of folate that can be used as a folate food supplement.
    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-10820AR
    Pemetrexed (disodium) (Standard)
    Pemetrexed (disodium) (Standard) is the analytical standard of Pemetrexed (disodium). This product is intended for research and analytical applications. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed (disodium) (Standard)
  • 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