2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Antifolate

Antifolate

Antifolate

Related Products

PDF 0.19 MB

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 (124):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1902
    Diaveridine
    		99.79%
    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
  • HY-139743
    Aditoprime
    		99.68%
    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
  • HY-10824
    Talotrexin
    		99.27%
    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-B0510S2
    Trimethoprim-d3
    		98.24%
    Trimethoprim-d3is the deuterium labeled Trimethoprim. 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 urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment[1][2][3].
    Trimethoprim-d<sub>3</sub>
  • HY-137439
    Fanotaprim
    		98.89%
    Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis.
    Fanotaprim
  • HY-12784S
    Cycloguanil-d6
    		≥98.0%
    Cycloguanil-d66 is the deuterium labeled Cycloguanil, which is a dihydrofolate reductase inhibitor.
    Cycloguanil-d<sub>6</sub>
  • HY-B0806AS1
    Proguanil-d6 hydrochloride
    		98.73%
    Proguanil-d6 hydrochloride is the deuterium labeled Proguanil hydrochloride (HY-B0806A). Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil-d6 hydrochloride
  • 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-13617
    Edatrexate
    Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck.
    Edatrexate
  • HY-B0806A
    Proguanil hydrochloride
    		99.21%
    Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil hydrochloride
  • HY-135101
    Methotrexate γ-Methyl Ester
    		Control 98.30%
    Methotrexate γ-Methyl Ester (Methotrexate 5-methyl ester) is an impurity of the folate antagonist Methotrexate (HY-14519).
    Methotrexate γ-Methyl Ester
  • 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-114306
    EC0489
    		Chemical
    EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor. Small molecule-agent conjugate (SMDC).
    EC0489
  • HY-14519D
    Methotrexate monohydrate
    Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, 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 monohydrate
  • HY-121151
    (±)-Methotrexate
    (±)-Methotrexate ((±)-Amethopterin) is a racemate of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of Folic acid into Tetrahydrofolate, and inhibiting DNA synthesis.
    (±)-Methotrexate
  • HY-128939
    EC0488
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
    EC0488
  • HY-B0806AS
    Proguanil-d4 hydrochloride
    Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor[1][2].
    Proguanil-d<sub>4</sub> hydrochloride
  • HY-108251S
    Methotrexate metabolite-d3
    Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent[1].
    Methotrexate metabolite-d<sub>3</sub>
  • HY-14523
    LY 254155
    LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
    LY 254155
  • HY-B0806S1
    Proguanil-d4
    Proguanil-d4 is the deuterium labeled Proguanil[1]. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor[2][3].
    Proguanil-d<sub>4</sub>