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 Antagonists
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Antifolate Modulator
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Antifolate Chemicals
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Antifolate Controls
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Antifolate Substrate
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Antifolate Ligand
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Antifolate Produits associés (150)
Produits associés (150)
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FR-β ligand 1
0 ImagesCat. No.: HY-172935CAS No.: 863869-78-7FR-β ligand 1 (III), a folate receptor-targeting ligand, possesses antitumor activity, high selectivity, and stronger affinity for folate receptor.
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10-Formylfolic acid-d4
0 ImagesCat. No.: HY-124350SCAS No.: 461426-41-510-Formylfolic acid-d4 is the deuterated-labeled 10-Formylfolic acid (HY-124350). 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase, with an IC50 of 80 nM against the rat enzyme. 10-Formylfolic acid also acts as an orally active folate source and a growth factor for specific bacteria. 10-Formylfolic acid supports growth and increases plasma folate levels; its absorption and metabolism patterns are similar to those of folic acid, but its liver retention is slightly higher. It exhibits high folate activity in microbial assays, serves as a growth factor for Enterococcus faecalis and Lactobacillus casei, aids folate nutrient supply, and may exert cell regulatory functions.
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Denopterin
0 ImagesCat. No.: HY-121207CAS No.: 22006-84-4Synonyms: Pteroylglutamic acidDenopterin is a dihydrofolate reductase (DHFR) inhibitor and an antifolate agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer.
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Mobiletrex
0 ImagesCat. No.: HY-121927CAS No.: 238074-89-0Synonyms: CH-1504Mobiletrex is an anti folate and dihydrofolate reductase inhibitor that can be used in research on rheumatoid arthritis.
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TNP-351
0 ImagesCat. No.: HY-19095CAS No.: 125991-51-7TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
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Proguanil hydrochloride (Standard)
0 ImagesCat. No.: HY-B0806ARCAS No.: 637-32-1Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
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Chlorasquin
0 ImagesCat. No.: HY-121256CAS No.: 18921-73-8Chlorasquin 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.
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(±)-Methotrexate-d3
0 ImagesCat. No.: HY-121151SSynonyms: (±)-Amethopterin-d3; (±)-CL14377-d3; (±)-WR19039-d3(±)-Methotrexate-d3 ((±)-Amethopterin-d3; (±)-CL14377-d3; (±)-WR19039-d3) is the deuterated-labeled (±)-Methotrexate (HY-121151). (±)-Methotrexate is the racemate of Methotrexate (HY-14519). Methotrexate 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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10-Formylfolic acid (Standard)
0 ImagesCat. No.: HY-124350RCAS No.: 134-05-410-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid (HY-124350). This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase, with an IC50 of 80 nM against the rat enzyme. 10-Formylfolic acid also acts as an orally active folate source and a growth factor for specific bacteria. 10-Formylfolic acid supports growth and increases plasma folate levels; its absorption and metabolism patterns are similar to those of folic acid, but its liver retention is slightly higher. It exhibits high folate activity in microbial assays, serves as a growth factor for Enterococcus faecalis and Lactobacillus casei, aids folate nutrient supply, and may exert cell regulatory functions.
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Pemetrexed-d5 disodium
0 ImagesCat. No.: HY-10820ASSynonyms: LY231514-d5 disodiumPemetrexed-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.
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AG2034
0 ImagesCat. No.: HY-10819CAS No.: 177575-17-6AG2034 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.
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FRα-IN-1
0 ImagesCat. No.: HY-147699CAS No.: 2028296-64-0FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
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(R)-Pralatrexate
0 ImagesCat. No.: HY-117791CAS No.: 1320211-70-8(R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor.
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Cycloguanil-d6 nitrate
0 ImagesCat. No.: HY-12784S1CAS No.: 2070015-19-7Synonyms: Chlorguanide triazine-d6 nitrateCycloguanil-d6 (Chlorguanide triazine-d6) nitrate is the deuterium labeled Cycloguanil nitrate. Cycloguanil nitrate is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil nitrate blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil nitrate inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil nitrate also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
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(±)-Methotrexate
0 ImagesCat. No.: HY-121151CAS No.: 60388-53-6Synonyms: (±)-Amethopterin; (±)-CL14377; (±)-WR19039(±)-Methotrexate ((±)-Amethopterin; (±)-CL14377; (±)-WR19039) is the racemate of Methotrexate (HY-14519). Methotrexate 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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Talotrexin monoammonium
0 ImagesCat. No.: HY-10824ACAS No.: 648420-92-2Synonyms: PT523 monoammoniumTalotrexin 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.
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(±)-Methotrexate-13C,d3 disodium
0 ImagesCat. No.: HY-121151S2Synonyms: (±)-Amethopterin-13C,d3 disodium; (±)-CL14377-13C,d3 disodium; (±)-WR19039-13C,d3 disodium(±)-Methotrexate-13C,d3 disodium ((±)-Amethopterin-13C,d3 disodium; (±)-CL14377-13C,d3 disodium; (±)-WR19039-13C,d3 disodium) is the deuterated, 13C-labeled (±)-Methotrexate (HY-121151). (±)-Methotrexate is the racemate of Methotrexate (HY-14519). Methotrexate 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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Tetrahydroaminopterin
0 ImagesCat. No.: HY-117551CAS No.: 14231-41-5Synonyms: NSC 524120Tetrahydroaminopterin (NSC 524120) is a tetrahydropteridine analog and the tetrahydro-reduced derivative of aminopterin. Tetrahydroaminopterin is used for studies on phenylalanine hydroxylase cofactor binding and the structure-activity relationship of tetrahydrobiopterin analogs.
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UCP1173
0 ImagesCat. No.: HY-183053CAS No.: 1922152-09-7UCP1173, propargyl-linked antifolate, is an antibacterial agent. UCP1173 inhibits DHFR enzymes, with IC50 values of 0.014 μM for DfrB, 0.19 μM for DfrG, 0.27 μM for DfrA, and 0.091 μM for DfrK. UCP1173 inhibits growth of Staphylococcus aureus clinical isolates carrying dfrA, dfrG, or dfrK resistance genes. UCP1173 can be used for the research of bacterial infections.
