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Dihydrofolate reductase (DHFR)

" in MedChemExpress (MCE) Product Catalog:

65

Inhibitors & Agonists

2

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2

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7

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-137439

    VYR-006

    Antifolate Infection
    Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor with IC50s of 1.57 and 308 nM for tgDHFR (Toxoplasma gondii DHFR) and hDHFR (human DHFR), respectively. Fanotaprim has the potential for the research of toxoplasmosis .
    Fanotaprim
  • HY-E70522

    DHFR

    Others Others
    Dihydrofolate reductase is a key enzyme in folate metabolism and, therefore, in the production of thymidine. Its role in thymidine biosynthesis is the reduction of dihydrofolate to tetrahydrofolate using the cofactor NADPH .
    Dihydrofolate reductase
  • HY-169211

    Dihydrofolate reductase (DHFR) Cancer
    DHFR-IN-21 (compund 5p) is a dihydrofolate reductase (DHFR) inhibitor .
    DHFR-IN-21
  • 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-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-153007A

    Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-5 hydrochloride 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 hydrochloride shows anti-malaria activity .
    DHFR-IN-5 hydrochloride
  • HY-169790

    Dihydrofolate reductase (DHFR) Parasite Infection
    Phomarin is an inhibitor for dihydrofolate reductase (DHFR), and exhibits potential antimalarial activity .
    Phomarin
  • HY-149200

    Antifolate Inflammation/Immunology
    Lysine-methotrexate, an analogue of Methotrexate (HY-14519), is a dihydrofolate reductase (DHFR) inhibitor .
    Lysine-methotrexate
  • HY-161292

    Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-16 (compound 8d) is an inhibitor of dihydrofolate reductase (DHFR) (IC50=0.199 μM) and can be used in anti-infectious research .
    DHFR-IN-16
  • HY-I0447A
    Sodium 4-aminosalicylate dihydrate
    1 Publications Verification

    4-Aminosalicylic acid sodium salt dihydrate

    Bacterial Antibiotic Infection
    Sodium 4-aminosalicylate (Sodium para-Aminosalicylic acid) dihydrate is para-aminosalicylic acid (PAS), a dihydrofolate reductase (DHFR) inhibitor and antituberculous agent. PAS is incorporated into the folate pathway via dihydropteroate synthase (DHPS) and dihydrofolate synthase (DHFS) to generate the hydroxydihydrofolate antimetabolite, which in turn inhibits DHFR enzyme activity .
    Sodium 4-aminosalicylate dihydrate
  • HY-18062S

    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)[1][2].
    Pyrimethamine-d3
  • HY-B1902R

    Antifolate Bacterial Infection
    Diaveridine (Standard) is the analytical standard of Diaveridine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-151159

    Dihydrofolate reductase (DHFR) EGFR Cancer
    DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells .
    DHFR-IN-4
  • HY-147661

    Antifolate Infection
    DHFR-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 .
    DHFR-IN-2
  • 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-117791

    Others Cancer
    (R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor .
    (R)-Pralatrexate
  • HY-121207

    Pteroylglutamic acid

    Antifolate Nucleoside Antimetabolite/Analog Cancer
    Denopterin 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 .
    Denopterin
  • 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-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-149459A

    (E)-azoMTX

    Dihydrofolate reductase (DHFR) Cancer
    Phototrexate is a photoswitchable inhibitor of the human dihydrofolate reductase (DHFR). Phototrexate has antifolate and antiproliferative properties, which can be used for the research of cancer .
    Phototrexate
  • HY-B1902S

    EGIS-5645-d6

    Isotope-Labeled Compounds Antifolate Bacterial Infection
    Diaveridine-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 .
    Diaveridine-d6
  • 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-156122

    Dihydrofolate reductase (DHFR) Bacterial Infection
    DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection .
    DHFR-IN-8
  • HY-143408

    Bacterial Infection
    OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains .
    OYYF-175
  • 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-143236

    Bacterial Fungal Infection
    DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249 .
    DHFR-IN-1
  • HY-I0447AR

    Bacterial Antibiotic Infection
    Sodium 4-aminosalicylate (dihydrate) (Standard) is the analytical standard of Sodium 4-aminosalicylate (dihydrate). This product is intended for research and analytical applications. Sodium 4-aminosalicylate (Sodium para-Aminosalicylic acid) dihydrate is para-aminosalicylic acid (PAS), a dihydrofolate reductase (DHFR) inhibitor and antituberculous agent. PAS is incorporated into the folate pathway via dihydropteroate synthase (DHPS) and dihydrofolate synthase (DHFS) to generate the hydroxydihydrofolate antimetabolite, which in turn inhibits DHFR enzyme activity .
    Sodium 4-aminosalicylate (dihydrate) (Standard)
  • HY-139743

    Aditoprim

    Antifolate Bacterial Infection
    Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics .
    Aditoprime
  • HY-118251

    Antifolate Dihydrofolate reductase (DHFR) Cancer
    PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
    PD130883
  • HY-B0806AS

    Isotope-Labeled Compounds Parasite Antifolate Infection
    Proguanil-d4 (hydrochloride) is the deuterium labeled Proguanil hydrochloride. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor[1][2].
    Proguanil-d4 hydrochloride
  • HY-159899

    Bacterial Antibiotic Dihydrofolate reductase (DHFR)
    DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase) inhibitor belonging to the class of 2,4-diaminopyrimidine compounds. DHFR-IN-22 exhibits significant inhibitory activity against purified DHFR enzyme and major species of nontuberculous mycobacteria (NTM), namely Mycobacterium avium and Mycobacterium abscessus. It shows an IC50 of 1.1 nM and MIC of 1.5 μg/mL against M. abscessus, and an IC50 of 6.3 nM and MIC of 0.1 μg/mL against M. avium. Additionally, it demonstrates an IC50 of 2100 nM against human DHFR. DHFR-IN-22 holds potential for studying novel strategies to combat NTM infections .
    DHFR-IN-22
  • HY-10373
    Trimetrexate
    2 Publications Verification

    CI-898

    Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Infection Cancer
    Trimetrexate (CI-898) 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 can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer .
    Trimetrexate
  • HY-10373A

    CI-898 trihydrochloride

    Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Infection Cancer
    Trimetrexate (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 .
    Trimetrexate trihydrochloride
  • HY-18062R

    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-10820B
    Pemetrexed disodium heptahydrate
    Maximum Cited Publications
    27 Publications Verification

    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-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-13781
    Pemetrexed disodium hemipenta hydrate
    Maximum Cited Publications
    27 Publications Verification

    LY231514 disodium hemipenta hydrate

    Antifolate Autophagy Apoptosis Cancer
    Pemetrexed disodium hemipenta hydrate 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 hemipenta hydrate
  • HY-168069

    Parasite Dihydrofolate reductase (DHFR) Infection
    DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
    DHFR-IN-20
  • HY-B0806S1

    Antifolate Parasite Infection
    Proguanil-d4 is the deuterium labeled Proguanil[1]. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor[2][3].
    Proguanil-d4
  • HY-111202R

    Cytochrome P450 Inflammation/Immunology
    Proguanil (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 .
    Pyributicarb (Standard)
  • HY-B0806R

    Parasite Antifolate Infection
    Proguanil (Standard) is the analytical standard of Proguanil. This product is intended for research and analytical applications. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor .
    Proguanil (Standard)
  • HY-10820
    Pemetrexed
    Maximum Cited Publications
    27 Publications Verification

    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-B0806AR

    Parasite Antifolate Infection
    Proguanil (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 .
    Proguanil (hydrochloride) (Standard)
  • HY-10373B

    CI-898 isethionate

    Dihydrofolate reductase (DHFR) Antibiotic Antifolate Parasite Bacterial DNA/RNA Synthesis Infection Cancer
    Trimetrexate (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 .
    Trimetrexate isethionate
  • HY-10820A
    Pemetrexed disodium
    Maximum Cited Publications
    27 Publications Verification

    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-115836

    Dihydrofolate reductase (DHFR) Cancer
    DDPO is an inhibitor for dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. DDPO inhibits the cell growth of cancer cell L1210 and WI-L2with IC50 of 5 and 0.28 µM .
    DDPO
  • HY-139743R

    Antifolate Bacterial Infection
    Aditoprime (Standard) is the analytical standard of Aditoprime. This product is intended for research and analytical applications. Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics .
    Aditoprime (Standard)

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