Antifolate
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.
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Antifolate Inhibitors
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Antifolate Chemicals
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Antifolate Substrate
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Antifolate Related Products (149)
Related Products (149)
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Methotrexate hydrate
0 ImagesSynonyms: Amethopterin hydrate; CL14377 hydrate; WR19039 hydrateMethotrexate hydrate (Amethopterin hydrate; CL14377 hydrate; WR19039 hydrate) is an orally active antifolate (Antifolate). Methotrexate hydrate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate hydrate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate hydrate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate hydrate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.
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Proguanil
0 ImagesProguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
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Pemetrexed disodium hemipenta hydrate
0 ImagesSynonyms: LY231514 disodium hemipenta hydratePemetrexed (LY231514) disodium hemipenta hydrate is a CNS-penetrant 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.
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Folinic acid calcium salt pentahydrate
0 ImagesFolinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
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Levomefolate calcium
0 ImagesLevomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia.
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Trimethoprim-d9
0 ImagesTrimethoprim-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.
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Manninotriose
0 ImagesManninotriose is a natural functional trisaccharide composed of three mannose molecules. Manninotriose binds to dihydrofolate reductase via hydrogen bond formation with Arg28. Manninotriose binds to thymidylate synthase via hydrogen bond formation with Arg50. Manninotriose acts as a membrane protectant and helps improve stress tolerance. Manninotriose can be used in research related to acute lymphoblastic leukemia.
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Cycloguanil hydrochloride
0 ImagesCycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
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Rinatabart
0 ImagesSynonyms: F131; GEN1184 antibodyRinatabart (F131) is an IgG1-κ human antibody targeting FOLR1, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001). The Fc region of Rinatabart is engineered to reduce antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) activities. The KD values of Rinatabart binding to human FOLR1 in two sets of BLI assays are 1.528 nM and 5.296 nM, respectively. Rinatabart shows significantly lower affinity for FOLR2 and mouse FOLR1, and no reliable specific binding to FOLR3 and rat FOLR1. Rinatabart can be used in studies of FOLR1 targeting and antibody-drug conjugates.
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Metoprine
0 ImagesMetoprine (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.
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LSN 3213128
0 ImagesLSN 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. LSN 3213128 exhibits anti-tumor activity.
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Talotrexin
0 ImagesSynonyms: PT523Talotrexin (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.
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Pemetrexed disodium heptahydrate
0 ImagesSynonyms: LY231514 disodium heptahydratePemetrexed 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.
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Pemetrexed (Standard)
0 ImagesSynonyms: LY231514 (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.
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Methotrexate metabolite
0 ImagesSynonyms: DAMPAMethotrexate 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.
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Methotrexate (Standard)
0 ImagesSynonyms: Amethopterin (Standard); CL14377 (Standard); WR19039 (Standard)Methotrexate (Standard) (Amethopterin (Standard); CL14377 (Standard); WR19039 (Standard)) is the analytical standard of Methotrexate (HY-14519). This product is intended for research and analytical applications. Methotrexate (Amethopterin; CL14377; WR19039) is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.
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Trimethoprim (Standard)
0 ImagesTrimethoprim (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.
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LY309887
0 ImagesLY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
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Methotrexate-d3
0 ImagesMethotrexate-d3 is the deuterated-labeled Methotrexate (HY-14519). Methotrexate (Amethopterin; CL14377; WR19039) is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.
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Tetroxoprim
0 ImagesSynonyms: HE 781Tetroxoprim is an antimicrobial DHFR inhibitor.
