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 (122):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-B0510C
    Trimethoprim lactate
    		99.97%
    Trimethoprim lactate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim lactate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
    Trimethoprim lactate
  • HY-17383
    Levomefolate calcium
    		99.46%
    Levomefolate calcium is an orally active, BBB-penatrable and active form of folic acid. Levomefolate calcium can be used as a food supplement for folic acid and in the research of neural tube defect diseases.
    Levomefolate calcium
  • HY-129441
    Metoprine
    		99.90%
    Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
    Metoprine
  • HY-107981
    LSN 3213128
    		98.62%
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
    LSN 3213128
  • 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-108251
    Methotrexate metabolite
    		98.44%
    Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.
    Methotrexate metabolite
  • 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-13781
    Pemetrexed disodium hemipenta hydrate
    		99.78%
    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-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-14521A
    Lometrexol disodium
    		≥98.0%
    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-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-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-W003561
    DHFR-IN-3
    		Inhibitor 99.48%
    DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor with the IC50 values of 19 μM and 12 μM in rat liver and P. carinii DHFR, respectively.
    DHFR-IN-3
  • HY-107033
    Tetroxoprim
    		Inhibitor 99.32%
    Tetroxoprim is an antimicrobial DHFR inhibitor.
    Tetroxoprim
  • 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-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-17556S1
    Folinic acid-d4 calcium hydrate
    		Chemical
    Folinic acid-d4-1 (Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). 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-d<sub>4</sub> calcium hydrate
  • 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-133887
    Methotrexate α-tert-butyl ester
    Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.
    Methotrexate α-tert-butyl ester