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 (150)
Related Products (150)
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Diaveridine-d6
0 ImagesCat. No.: HY-B1902SSynonyms: EGIS-5645-d6Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. 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.
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Pemetrexed-d5
0 ImagesCat. No.: HY-10820SCAS No.: 1129408-57-6Synonyms: LY231514-d5Pemetrexed-d5 is the deuterium labeled Pemetrexed. 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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LY243246
0 ImagesCat. No.: HY-117058CAS No.: 106400-18-4Synonyms: (6S)-DDATHFLY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis.
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Antitumor agent-99
0 ImagesCat. No.: HY-157217Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. Antitumor agent-99 inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50s of 51.46 nM, 2.53 nM, and 2.98 nM, respectively.
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AGF347
0 ImagesCat. No.: HY-177092CAS No.: 2294820-23-6AGF347 is a potent and multi-targeted antifolate that targets serine hydroxymethyltransferase (SHMT)2 in the mitochondria and SHMT1 in the cytosol, and inhibits de novo purine biosynthesis. AGF347 induces apoptosis, inhibits mTOR signaling, decreases GSH pools, and increases ROS. AGF347 inhibits proliferation of Cisplatin (HY-17394) sensitive and resistant epithelial ovarian cancer (EOC) cells. AGF347 exhibits antitumor efficacy in SKOV3 EOC xenograft mouse models. AGF347 can be used for ovarian cancer research.
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Folinic acid calcium hydrate
0 ImagesCat. No.: HY-17556BCAS No.: 1097832-14-8Synonyms: Leucovorin calcium hydrateFolinic acid (Leucovorin) calcium hydrate is a biological folic acid and is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease Methotrexate-induced toxicity.
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Levomefolate-13C5 calcium
0 ImagesCat. No.: HY-17383SLevomefolate-13C5 calcium)is the 13C-labeled Levomefolate calcium (HY-17383). Levomefolate 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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DHFR-IN-2
0 ImagesCat. No.: HY-147661CAS No.: 331942-46-2DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research.
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Methotrexate metabolite (Standard)
0 ImagesCat. No.: HY-108251RCAS No.: 19741-14-1Synonyms: DAMPA (Standard)Methotrexate metabolite (Standard) is the analytical standard of Methotrexate metabolite. This product is intended for research and analytical applications. 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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Cycloguanil hydrochloride (Standard)
0 ImagesSynonyms: Chlorguanide triazine hydrochloride (Standard)Cycloguanil hydrochloride (Standard) is the analytical standard of Cycloguanil hydrochloride (HY-12784A). This product is intended for research and analytical applications. 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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Folinic acid disodium
0 ImagesCat. No.: HY-17556ACAS No.: 163254-40-8Synonyms: Leucovorin disodiumFolinic acid (Leucovorin) disodium is a biological folic acid and is a forms of vitamin B9. Folinic acid disodium is generally administered along with Methotrexate (HY-14519) as a rescue agent to decrease MTX-induced toxicity. Folinic acid disodium and Sfluorouracil adjuvant chemotherapy shows effective in colon carcinoma.
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Trimethoprim sulfate
0 ImagesCat. No.: HY-B0510ACAS No.: 56585-33-2Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc.
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Pralatrexate-13C5,15N
0 ImagesCat. No.: HY-10446S1Pralatrexate-13C5,15N is the 13C- and 15N-labeled Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Trimetrexate isethionate
0 ImagesCat. No.: HY-10373BCAS No.: 82935-04-4Synonyms: CI-898 isethionateTrimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
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10-Methyl-10-deazaaminopterin
0 ImagesCat. No.: HY-137267CAS No.: 80576-77-810-Methyl-10-deazaaminopterin is a folate analog and an antifolate. 10-Methyl-10-deazaaminopterin can be used for the research of cancer.
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Trimetrexate trihydrochloride
0 ImagesCat. No.: HY-10373ACAS No.: 1658520-97-8Synonyms: CI-898 trihydrochlorideTrimetrexate (CI-898) trihydrochloride is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate trihydrochloride can also inhibit the growth of various cancer cells. Trimetrexate trihydrochloride can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.
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Talotrexin ammonium
0 ImagesCat. No.: HY-10824BCAS No.: 678991-55-4Synonyms: PT523 ammoniumTalotrexin ammonium is a nonpolyglutamatable antifolate. Talotrexin ammonium improves antitumor activity in a broad spectrum of cancer models by targeting DHFR to inhibit tumor growth.
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LY 222306
0 ImagesCat. No.: HY-14522CAS No.: 154446-98-7LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
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Manninotriose (Standard)
0 ImagesCat. No.: HY-N0913RCAS No.: 13382-86-0Wy-45494 (hydrochloride) (Standard) is the analytical standard of Wy-45494 (hydrochloride). This product is intended for research and analytical applications. Wy-45494 hydrochloride (N-Desmethyl Venlafaxine hydrochloride; Wy 45494) is a minor active metabolite of the selective norepinephrine and serotonin reuptake inhibitor (SNRI) venlafaxine. It is formed from venlafaxine via the cytochrome P450 (CYP) isomer CYP3A4.2. Wy-45494 hydrochloride inhibits norepinephrine and serotonin reuptake in rat synaptosomal preparations (IC50s of 4.7 and 1.6 μM, respectively). In vivo, Wy-45494 hydrochloride reversed reserpine-induced hypothermia in mice at a minimum effective dose (MED) of 10 mg/kg.
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Sulfathiourea
0 ImagesSulfathiourea is an inhibitor of Pneumocystis carinii dihydropteroate synthetase (dihydropteroate synthetase), with an IC50 of 0.022 μM and a Ki of 16.5 nM. Sulfathiourea blocks folate biosynthesis by inhibiting the enzyme that links 7,8-dihydro-6-hydroxymethylpterin pyrophosphate with p-aminobenzoic acid to form dihydropteroate. Sulfathiourea can be used in research related to *Pneumocystis carinii* pneumonia.
