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 (72):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17383
    Levomefolate calcium
    		Chemical 99.29%
    Levomefolate calcium is an artificial form of folate.
    Levomefolate calcium
  • HY-14530
    Pelitrexol
    		98.94%
    Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice.
    Pelitrexol
  • HY-108251
    Methotrexate metabolite
    		98.22%
    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 is an antimalarial agent, which inhibits the parasite growth with an IC50 of 446 nM against the antifolate-sensitive strain and 812 nM against the highly resistant strain under physiological folate conditions. Methotrexate metabolite is inactive against mammalian cells. Methotrexate metabolite is a minimal inhibitor of dihydrofolate reductase among metabolites of methotrexate .
    Methotrexate metabolite
  • HY-14521B
    Lometrexol hydrate
    		99.20%
    Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    Lometrexol hydrate
  • HY-13781
    Pemetrexed disodium hemipenta hydrate
    		99.72%
    Pemetrexed disodium hemipenta hydrate 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 hemipenta hydrate
  • HY-10820B
    Pemetrexed disodium heptahydrate
    		Inhibitor 99.97%
    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
  • HY-14521A
    Lometrexol disodium
    Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    Lometrexol disodium
  • 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-103396
    Trimetrexate glucuronate
    		Antagonist 98.09%
    Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.
    Trimetrexate glucuronate
  • HY-B0510S
    Trimethoprim-d9
    		98.81%
    Trimethoprim-d9 is 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>9</sub>
  • HY-107033
    Tetroxoprim
    		Inhibitor 98.96%
    Tetroxoprim is an antimicrobial DHFR inhibitor.
    Tetroxoprim
  • HY-18062S
    Pyrimethamine-d3
    		99.90%
    Pyrimethamine-d3 is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR)[1][2].
    Pyrimethamine-d<sub>3</sub>
  • 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-10818
    LY309887
    		98.03%
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
    LY309887
  • HY-17557
    Calcium N5-methyltetrahydrofolate
    		Chemical 98.56%
    Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
    Calcium N5-methyltetrahydrofolate
  • 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-14519S
    Methotrexate-d3
    		≥99.0%
    Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. 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)[1][2][3].
    Methotrexate-d<sub>3</sub>
  • 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-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-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