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-121256
    Chlorasquin
    		Chemical
    Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
    Chlorasquin
  • HY-162975
    NVP-EVS459 (175Lu)
    		Chemical
    NVP-EVS459 (175Lu) is a folate receptor targeting radio-conjugate, and can be used for cancer research.
    NVP-EVS459 (175Lu)
  • HY-124350R
    10-Formylfolic acid (Standard)
    		Inhibitor
    10-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid. This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid (Standard)
  • HY-10820AS
    Pemetrexed-d5 disodium
    Pemetrexed-d5 (disodium) is the deuterium labeled Pemetrexed disodium. 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[1].
    Pemetrexed-d<sub>5</sub> disodium
  • HY-B0510B
    Trimethoprim hydrochloride
    Trimethoprim 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.
    Trimethoprim hydrochloride
  • HY-10819
    AG2034
    AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED.
    AG2034
  • HY-147699
    FRα-IN-1
    		Chemical
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
    FRα-IN-1
  • HY-12784S1
    Cycloguanil-d6 nitrate
    Cycloguanil-d6 (nitrate) is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
    Cycloguanil-d<sub>6</sub> nitrate
  • HY-10824A
    Talotrexin monoammonium
    Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin monoammonium
  • HY-17383R
    Levomefolate (calcium) (Standard)
    		Chemical
    Levomefolate (calcium) (Standard) is the analytical standard of Levomefolate (calcium). This product is intended for research and analytical applications. Levomefolate calcium is an orally active, blood-brain barrier-crossing form of folate that can be used as a folate food supplement.
    Levomefolate (calcium) (Standard)
  • HY-149200
    Lysine-methotrexate
    Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor.
    Lysine-methotrexate
  • HY-B1902S
    Diaveridine-d6
    Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. 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-d<sub>6</sub>
  • HY-B0806R
    Proguanil (Standard)
    Proguanil (Standard) is the analytical standard of Proguanil. This product is intended for research and analytical applications. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil (Standard)
  • HY-105934A
    Ketotrexate sodium
    Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases.
    Ketotrexate sodium
  • HY-10820R
    Pemetrexed (Standard)
    Pemetrexed (Standard) is the analytical standard of Pemetrexed. This product is intended for research and analytical applications. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed (Standard)
  • HY-13664R
    Folinic acid calcium (Standard)
    		Chemical
    Folinic acid (calcium) (Standard) is the analytical standard of Folinic acid (calcium). This product is intended for research and analytical applications. Folinic acid calcium (Leucovorin calcium) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
    Folinic acid calcium (Standard)
  • HY-124350
    10-Formylfolic acid
    		Inhibitor
    10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid
  • HY-B0510R
    Trimethoprim (Standard)
    Trimethoprim (Standard) is the analytical standard of Trimethoprim. This product is intended for research and analytical applications. 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 (Standard)
  • HY-126878
    11-Oxahomoaminopterin
    		Chemical
    11-Oxahomoaminopterin shows antifolate activity and inhibits Lactobacillus casei DHFFZ with antimicrobial and antitumor activities.
    11-Oxahomoaminopterin
  • HY-122259
    AMPte-Glu-γ-Glu
    		Inhibitor
    AMPte-Glu-γ-Glu is a substrate for folylpoly-γ-glutamate synthetase (FPGS). AMPte-Glu-γ-Glu exhibits cytotoxicity against chinese hamster ovaries cells, with IC50s of 20, 350 and 3 nM, for Pro3, R2, and 43-10, respectively.
    AMPte-Glu-γ-Glu