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 Related Products (145)
Related Products (145)
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Antifolate agent 1
0 ImagesCat. No.: HY-175428CAS No.: 518063-75-7Antifolate agent 1 is a 6-substituted pyrrolopyrimidine antifolate with a 1-carbon bridge. Antifolate agent 1 shows no activity against cells expressing FRα and FRβ, and has no GARFTase inhibitory activity. Antifolate agent 1 can be used as a negative control in the development of folate receptor-targeted antifolates.
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Cycloguanil-d6
0 ImagesSynonyms: Chlorguanide triazine-d6Cycloguanil-d6 (Chlorguanide triazine-d6) is the deuterium labeled Cycloguanil (HY-12784). Cycloguanil is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil 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 also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
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Proguanil-d6 hydrochloride
0 ImagesCat. No.: HY-B0806AS1Purity: 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.
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Lometrexol hydrate
0 ImagesSynonyms: DDATHF hydrateLometrexol (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.
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FRα-targeting peptide C7
0 ImagesCat. No.: HY-P10501CAS No.: 2159055-74-8FRα-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.
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Edatrexate
0 ImagesCat. No.: HY-13617CAS No.: 80576-83-6Synonyms: CGP 30694Edatrexate (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.
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Trimethoprim lactate (Standard)
0 ImagesActein (Standard) is the analytical standard of Actein. This product is intended for research and analytical applications. Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo.
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Opugotamig
0 ImagesSynonyms: IMGN-151 AntibodyHY-P990935 is an FOLR1-targeting half-IG G1 -κ/(scFv -κ-heavy) -h-CH2-CH3 type chimeric antibody.
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Methotrexate monohydrate
0 ImagesSynonyms: Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrateMethotrexate (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).
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(±)-Methotrexate
0 ImagesCat. No.: HY-121151CAS No.: 60388-53-6Synonyms: (±)-Amethopterin; (±)-CL14377; (±)-WR19039(±)-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.
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EC0488
0 ImagesCat. No.: HY-128939CAS No.: 1059477-92-7EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
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Cycloguanil-d4 (hydrochloride)
0 ImagesCat. No.: HY-12784ASCAS No.: 1189427-23-3Synonyms: Chlorguanide triazine-d4 hydrochlorideCycloguanil-d4 (Chlorguanide triazine-d4) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil 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 hydrochloride 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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Methotrexate metabolite-d3
0 ImagesCat. No.: HY-108251SCAS No.: 1794780-00-9Synonyms: DAMPA-d3Methotrexate 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.
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LY 254155
0 ImagesCat. No.: HY-14523CAS No.: 135503-67-2LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
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Proguanil-d4
0 ImagesCat. No.: HY-B0806S1CAS No.: 1189805-15-9Proguanil-d4 is the deuterium labeled Proguanil. Proguanil, 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-13C5
0 ImagesCat. No.: HY-W769288Synonyms: LY231514 disodium-13C5Pemetrexed disodium-13C5 (LY231514 disodium-13C5) is the 13C-labeled Pemetrexed disodium (HY-10820A). 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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Cycloguanil-d6 (hydrochloride)
0 ImagesCat. No.: HY-12784AS1CAS No.: 2712364-69-5Synonyms: Chlorguanide triazine-d6 hydrochlorideCycloguanil-d6 (Chlorguanide triazine-d6) hydrochloride is the deuterium labeled Cycloguanil hydrochloride (HY-12784A). Cycloguanil 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 hydrochloride 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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Aminopterin sodium
0 ImagesCat. No.: HY-14518ACAS No.: 58602-66-7Synonyms: 4-Aminofolic acid sodium; APGA sodiumAminopterin sodium (4-Aminofolic acid sodium) is an anti-tumor drug with immunosuppressive activity. Aminopterin sodium blocks the metabolism of folic acid by inhibiting the activity of dihydrofolate reductase, thereby affecting nucleic acid synthesis. Aminopterin sodium is mainly used to inhibit acute lymphoblastic leukemia and certain other types of cancer. Aminopterin sodium is also used clinically as an immunosuppressant to suppress autoimmune diseases.
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(R)-Methotrexate-d3
0 ImagesCat. No.: HY-14519CSCAS No.: 2470329-38-3(R)-Methotrexate-d3 is the deuterium labeled (R)-Methotrexate.
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Lysine-methotrexate
0 ImagesCat. No.: HY-149200CAS No.: 80407-56-3Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor.
