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Dihydrofolate Reductase Inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14519
    Methotrexate
    Maximum Cited Publications
    76 Publications Verification

    Amethopterin; CL14377; WR19039

    Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial Infection Neurological Disease Inflammation/Immunology Cancer
    Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, 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) .
    Methotrexate
  • HY-10820
    Pemetrexed
    35+ Cited Publications

    LY231514

    Antifolate Autophagy Cancer
    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 .
    Pemetrexed
  • HY-18062
    Pyrimethamine
    10+ Cited Publications

    Pirimecidan; Pirimetamin; RP 4753

    Antifolate Parasite Infection Cancer
    Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate .
    Pyrimethamine
  • HY-10820A
    Pemetrexed disodium
    35+ Cited Publications

    LY231514 disodium

    Antifolate Autophagy Apoptosis Cancer
    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 .
    Pemetrexed disodium
  • HY-B0510
    Trimethoprim
    10+ Cited Publications

    Antifolate Bacterial Antibiotic Influenza Virus Infection Cancer
    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 .
    Trimethoprim
  • HY-14519A
    Methotrexate disodium
    Maximum Cited Publications
    76 Publications Verification

    Amethopterin disodium; CL14377 disodium; WR19039 disodium

    Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial Inflammation/Immunology Cancer
    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, 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) .
    Methotrexate disodium
  • HY-I0447
    4-Aminosalicylic acid
    1 Publications Verification

    Antibiotic Bacterial Infection Inflammation/Immunology
    4-Aminosalicylic acid is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. 4-Aminosalicylic acid exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). 4-Aminosalicylic acid is orally active .
    4-Aminosalicylic acid
  • HY-13781

    LY231514 disodium hemipenta hydrate

    Antifolate Autophagy Apoptosis Infection Neurological Disease Inflammation/Immunology Cancer
    Pemetrexed (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.
    Pemetrexed disodium hemipenta hydrate
  • HY-14518

    4-Aminofolic acid; APGA

    Antifolate Inflammation/Immunology Cancer
    Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
    Aminopterin
  • HY-10820B
    Pemetrexed disodium heptahydrate
    35+ Cited Publications

    LY231514 disodium heptahydrate

    Antifolate Autophagy Cancer
    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-B0806
    Proguanil
    3 Publications Verification

    Parasite Antifolate Infection
    Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
    Proguanil
  • HY-B0510S

    Antifolate Bacterial Antibiotic Infection
    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 .
    Trimethoprim-d9
  • HY-B0806A
    Proguanil hydrochloride
    3 Publications Verification

    Parasite Antifolate Infection
    Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor .
    Proguanil hydrochloride
  • HY-153007

    Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .
    DHFR-IN-5
  • HY-10820R

    LY231514 (Standard)

    Reference Standards Antifolate Autophagy Cancer
    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 .
    Pemetrexed (Standard)
  • HY-I0447A
    Sodium 4-aminosalicylate dihydrate
    1 Publications Verification

    4-Aminosalicylic acid sodium salt dihydrate

    Antibiotic Bacterial Infection Inflammation/Immunology
    Sodium 4-aminosalicylate dihydrate (4-Aminosalicylic acid sodium salt dihydrate) is an inhibitor for dihydrofolate reductase (DHFR) and an antituberculous agent. Sodium 4-aminosalicylate dihydrate exhibits anti-inflammatory activity and can be used in research of inflammatory bowel disease (IBD). Sodium 4-aminosalicylate dihydrate is orally active .
    Sodium 4-aminosalicylate dihydrate
  • HY-B1902

    EGIS-5645

    Antifolate Bacterial Infection
    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-162475

    Dihydrofolate reductase (DHFR) Bacterial Infection
    Fluorofolin is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.5 nM. Fluorofolin exhibits significant activity against P. aeruginosa .
    Fluorofolin
  • HY-101479
    Iclaprim
    3 Publications Verification

    AR-100

    Bacterial Antibiotic Infection
    Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
    Iclaprim
  • HY-130569

    Drug Metabolite Inflammation/Immunology Cancer
    7-Hydroxymethotrexate is a major metabolite 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 .
    7-Hydroxymethotrexate
  • HY-169790

    Dihydrofolate reductase (DHFR) Parasite Fungal Infection
    Phomarin is an inhibitor for dihydrofolate reductase (DHFR). Phomarin exhibits activity against Plasmodium parasites and fungi including Mycrobotryum violaceum and Botrytis cinerea. Phomarin can be used for the research of malaria and fungal infections .
    Phomarin
  • HY-124350

    Antifolate Dihydrofolate reductase (DHFR) Cancer
    10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia .
    10-Formylfolic acid
  • HY-W003561

    Antifolate Parasite Infection
    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-106434

    BW 301U; NSC 351521

    Dihydrofolate reductase (DHFR) Infection Cancer
    Piritrexim (BW 301U) is a potent dihydrofolate reductase (DHFR) inhibitor against Pneumocystis carinii and Toxoplasma gondii, with IC50 values of 0.038 and 0.011 μM, respectively. Piritrexim can be used for acquired immune deficiency syndrome (AIDS) research. Piritrexim also is an anticancer agent .
    Piritrexim
  • HY-14519R

    Amethopterin (Standard); CL14377 (Standard); WR19039 (Standard)

    Reference Standards Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial Inflammation/Immunology Cancer
    Methotrexate (Standard) is the analytical standard of Methotrexate. This product is intended for research and analytical applications. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, 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) .
    Methotrexate (Standard)
  • HY-121341

    Ro 10-5970

    Bacterial Infection
    Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria .
    Brodimoprim
  • HY-133624
    1,1,3-Tribromoacetone
    1 Publications Verification

    Drug Metabolite Cancer
    1,1,3-Tribromoacetone is an impurity 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 .
    1,1,3-Tribromoacetone
  • HY-116387A
    WR99210 hydrochloride
    4 Publications Verification

    BRL 6231

    Dihydrofolate reductase (DHFR) Parasite Infection
    WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii .
    WR99210 hydrochloride
  • HY-B0510B
    Trimethoprim hydrochloride
    10+ Cited Publications

    Antifolate Bacterial Antibiotic Influenza Virus Infection Cancer
    Trimethoprim hydrochloride is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim hydrochloride is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
    Trimethoprim hydrochloride
  • HY-103396
    Trimetrexate glucuronate
    2 Publications Verification

    CI-898 glucuronate

    Antifolate Bacterial Infection Cancer
    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-18062R

    Pirimecidan (Standard); Pirimetamin (Standard); RP 4753 (Standard)

    Reference Standards Antifolate Parasite Infection
    Pyrimethamine (Standard) is the analytical standard of Pyrimethamine. This product is intended for research and analytical applications. Pyrimethamine (Pirimecidan) is a potent, orally active dihydrofolate reductase (DHFR) inhibitor. Pyrimethamine is an antimalarial agent. Pyrimethamine affects the nucleoprotein metabolism of malarial parasites by interference in the folic–folinic acid systems and affects cell division by inhibiting the conversion of dihydrofolate to tetrahydrofolate .
    Pyrimethamine (Standard)
  • HY-19581

    Antibiotic Bacterial Infection
    Baquiloprim, an antibiotic, is a selective inhibitor of bacterial dihydrofolate reductases. Baquiloprim possesses in vitro bacteriostatic activity against both Gram-negative and Gram-positive bacteria .
    Baquiloprim
  • HY-139743

    Aditoprim

    Antifolate Bacterial Infection
    Aditoprime (Aditoprim) is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR, respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
    Aditoprime
  • HY-179415

    Dihydrofolate reductase (DHFR) Bacterial Infection
    DHFR-IN-24, a benzothiazole derivative, is a dihydrofolate reductase (DHFR) inhibitor. DHFR-IN-24 has intrinsic antibacterial activity against both Gram-positive and Gram-negative strains. DHFR-IN-24 synergistically combines DHFR inhibition with photodynamic therapy (PDT) for enhanced antibacterial activity against multidrug-resistant pathogens .
    DHFR-IN-24
  • HY-149200

    Antifolate Inflammation/Immunology
    Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor .
    Lysine-methotrexate
  • HY-121151

    (±)-Amethopterin; (±)-CL14377; (±)-WR19039

    Antifolate Others
    (±)-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 .
    (±)-Methotrexate
  • HY-160254

    Dihydrofolate reductase (DHFR) Cancer
    1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity .
    1954U89
  • HY-116039

    Ro11-8958

    Dihydrofolate reductase (DHFR) Bacterial Infection
    Epiroprim (Ro11-8958) is a selective dihydrofolate reductase (DHFR) inhibitor. Epiroprim displays excellent activity against staphylococci, enterococci, pneumococci, and streptococci .
    Epiroprim
  • HY-18062S

    Isotope-Labeled Compounds Antifolate Parasite Infection
    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) .
    Pyrimethamine-d3
  • HY-B0806S1

    Antifolate Parasite Infection
    Proguanil-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 .
    Proguanil-d4
  • HY-19095

    Antifolate Cancer
    TNP-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 .
    TNP-351
  • HY-14519D

    Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate

    Antifolate DNA/RNA Synthesis ADC Payload Apoptosis Bacterial Inflammation/Immunology Cancer
    Methotrexate (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) .
    Methotrexate monohydrate
  • HY-122289

    Dihydrofolate reductase (DHFR) Bacterial Infection
    Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
    Metioprim
  • HY-16638

    PDDF

    Thymidylate Synthase Metabolic Disease
    CB 3717 is a potent inhibitor of human thymidylate synthetase, competitively binding with 5,10-methylenetetrahydrofolate (Ki = 4.9 X 10(-9) M). It also competitively inhibits human dihydrofolate reductase with dihydrofolate (Ki = 2.3 X 10(-8) M). In WI-L2 human lymphoblastoid cells, CB 3717 treatment led to a significant decrease in cellular dTTP levels and a notable increase in dUMP levels, indicating a disruption in nucleotide metabolism. The growth-inhibitory effect of CB 3717 was reversed by thymidine supplementation, demonstrating that thymidylate synthetase became rate-limiting in the presence of this compound. Delayed thymidine supplementation beyond 8 hours resulted in severe cytotoxicity, underscoring the critical timing of nucleotide rescue strategies in CB 3717-treated cells .
    CB 3717
  • HY-124350R

    Antifolate Reference Standards Dihydrofolate reductase (DHFR) Cancer
    10-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid. This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia .
    10-Formylfolic acid (Standard)
  • HY-139743R

    Aditoprim (Standard)

    Reference Standards Antifolate Bacterial Infection
    Aditoprime (Standard) is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR, respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
    Aditoprime (Standard)
  • HY-177337

    N-Didesmethyl-ADP

    Drug Metabolite Antifolate Bacterial Infection
    N-Didesmethyladitoprim is a metabolite of Aditoprime (HY-139743). Aditoprime is a selective bacterial dihydrofolate reductase (DHFR) inhibitor with IC50s of 47 and 520 nM for E.coli and L.casei DHFR , respectively. Aditoprime inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime has a broad-spectrum antibacterial activity and excellent pharmacokinetics .
    N-Didesmethyladitoprim
  • HY-161063

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-14 (compound 32) is a pyrimethamine (Pyr)-type, dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity .
    DHFR-IN-14
  • HY-161064

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM .
    DHFR-IN-15
  • HY-169211

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-21 (compund 5p) is a dihydrofolate reductase (DHFR) inhibitor .
    DHFR-IN-21

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