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-157217
    Antitumor agent-99
    		Inhibitor
    Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. Antitumor agent-99 inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50s of 51.46 nM, 2.53 nM, and 2.98 nM, respectively.
    Antitumor agent-99
  • HY-17556B
    Folinic acid calcium hydrate
    		Chemical
    Folinic acid (Leucovorin) calcium hydrate 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 calcium hydrate
  • HY-17383S
    Levomefolate-13C5 calcium
    		Chemical
    Levomefolate-13C5 (calcium) is the 13C-labeled Levomefolate (calcium). Levomefolate calcium is an artificial form of folate.
    Levomefolate-<sup>13</sup>C<sub>5</sub> calcium
  • HY-10824
    Talotrexin
    Talotrexin (PT523), an analog of Aminopterin (HY-14518), is a nonpolyglutamatable classic antifolate. Talotrexin is a RFC (reduced folate carrier) specific inhibitor and selectively inhibits RFC transport. Talotrexin shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin
  • HY-10820BR
    Pemetrexed (disodium heptahydrate) (Standard)
    		Inhibitor
    Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. Pemetrexed disodium heptahydrate 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 heptahydrate) (Standard)
  • HY-147661
    DHFR-IN-2
    		Inhibitor
    DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research.
    DHFR-IN-2
  • HY-108251R
    Methotrexate metabolite (Standard)
    Methotrexate metabolite (Standard) is the analytical standard of Methotrexate metabolite. This product is intended for research and analytical applications. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent.
    Methotrexate metabolite (Standard)
  • HY-17556A
    Folinic acid disodium
    		Chemical
    Folinic acid (Leucovorin) disodium is a biological folic acid and is a forms of vitamin B9. Folinic acid disodium is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity. Folinic acid disodium and Sfluorouracil adjuvant chemotherapy shows effective in colon carcinoma.
    Folinic acid disodium
  • HY-B0510A
    Trimethoprim sulfate
    Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
    Trimethoprim sulfate
  • HY-10373B
    Trimetrexate isethionate
    Trimetrexate (CI-898) isethionate 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 isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
    Trimetrexate isethionate
  • HY-137267
    10-Methyl-10-deazaaminopterin
    10-Methyl-10-deazaaminopterin is a folate analog and an antifolate. 10-Methyl-10-deazaaminopterin can be used for the research of cancer.
    10-Methyl-10-deazaaminopterin
  • HY-10373A
    Trimetrexate trihydrochloride
    Trimetrexate (CI-898) trihydrochloride 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 trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
    Trimetrexate trihydrochloride
  • HY-10824B
    Talotrexin ammonium
    Talotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth.
    Talotrexin ammonium
  • HY-14522
    LY 222306
    LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
    LY 222306
  • HY-P10501
    FRα-targeting peptide C7
    FRα-targeting peptide C7 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 can be used in the research of tumor diagnosis and treatment.
    FRα-targeting peptide C7
  • HY-121207
    Denopterin
    		Inhibitor
    Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an antifolate agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer.
    Denopterin
  • HY-121927
    Mobiletrex
    Mobiletrex is an anti folate and dihydrofolate reductase inhibitor that can be used in research on rheumatoid arthritis.
    Mobiletrex
  • HY-17557R
    Calcium N5-methyltetrahydrofolate (Standard)
    		Chemical
    Calcium N5-methyltetrahydrofolate (Standard) is the analytical standard of Calcium N5-methyltetrahydrofolate. This product is intended for research and analytical applications. 0
    Calcium N5-methyltetrahydrofolate (Standard)
  • HY-19095
    TNP-351
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
    TNP-351
  • HY-B0806AR
    Proguanil (hydrochloride) (Standard)
    Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil (hydrochloride) (Standard)