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TargetMol | Tags Cell Cycle/Checkpoint
TargetMol | Tags DNA Damage/DNA Repair
TargetMol | Tags Metabolism

DHFR

Dihydrofolate reductase, or DHFR, is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, using NADPH as electron donor, which can be converted to the kinds of tetrahydrofolate cofactors used in 1-carbon transfer chemistry. In humans, the DHFR enzyme is encoded by the DHFR gene. It is found in the q11→q22 region of chromosome 5.[7] Bacterial species possess distinct DHFR enzymes (based on their pattern of binding diaminoheterocyclic molecules), but mammalian DHFRs are highly similar.

  • Methotrexate Diglutamate
    T2588641600-13-9In house
    Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.
    • $1,630
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  • Pemetrexed
    T0189137281-23-3
    Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
    • $33
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  • Urea
    T073857-13-6
    Urea (Carbonyldiamide) is formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end metabolite of protein catabolism and accounts for about one-half of the total urinary solids.
    • $30
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  • Trimethoprim
    T1153738-70-5
    Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor, and Cytochrome P450 2C8 Inhibitor, and Organic Cation Transporter 2 Inhibitor.
    • $45
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  • Gentamicin sulfate
    T13261405-41-0
    Gentamicin sulfate (SCH9724) is a wide-spectrum, aminoglycoside antibiotic used to inhibit protein synthesis in sensitive organisms.
    • $31
    In Stock
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  • Piritrexim
    T2464472732-56-0In house
    Piritrexim (BW 301U) is an orally available fat-soluble dihydrofolate reductase inhibitor with pulmonary toxicity used in the study of uroepithelial carcinoma and metastatic breast cancer.
    • $350
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  • P 218
    T73328L1142407-60-0In house
    P 218 is a novel DHFR inhibitor with antimalarial activity and antifolate effects and can be used to study Buruli ulcer.
    • $129
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  • 10-Formylfolic acid
    T24962134-05-4
    10-Formylfolic acid is a novel and potent inhibitor of dihydrofolate reductase, which can be used in leukemia research.
    • $392
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  • Talotrexin ammonium
    T64295648420-92-2In house
    Talotrexin ammonium is a non-polyglutamic acid antifolate. Talotrexin ammonium inhibits tumor growth by targeting dihydrofolate reductase (DHFR), thereby improving anti-tumor activity in a wide range of cancer models, helping to inhibit tumor growth.
    • $350
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  • DHFR-IN-4
    T614862820126-49-4
    DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumour activity, inhibits EGFR and HER2 and can be used to study pancreatic cancer.
    • $350
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  • Lometrexol
    T15826106400-81-1In house
    Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    • $98
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  • Pemetrexed disodium hemipenta hydrate
    T6226357166-30-4
    Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.
    • $33
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    TargetMol | Citations Cited
  • 4′-DTMP
    T7823821253-58-7
    4′-DTMP (4-Demethyltrimethoprim) is a potent DHFR inhibitor with antimicrobial activity that induces additional local interactions with the enzyme and inhibits Escherichia coli.
    • $30
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  • Fanotaprim
    T366922120282-75-7
    Fanotaprim is a dihydrofolate reductase (DHFR) inhibitor. Fanotaprim inhibits the growth of T. gondii strains with a TgDHFR IC50 of 1.57 ± 0.11 nM and a hDHFR IC50 of 308 ± 71 nM and a hDHFR to TgDHFR selectivity ratio of 196.
    • $80
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  • DHFR-IN-3
    T3693137553-43-6
    DHFR-IN-3 (7-bromoquinazoline-2,4-diamine) is a dihydrofolate reductase (DHFR) inhibitor.
    • $41
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  • Trioxsalen
    T45583902-71-4
    Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.
    • $29
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  • Pralatrexate
    T6120146464-95-1
    Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities.
    • $30
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  • Diaveridine
    T22045355-16-8
    Diaveridine (AI3-23935) (DVD) is a popular antibacterial synergist that is widely used in combination with sulfonamide. It has been reported to be genotoxic to mammalian cells, but more studies are required to clarify this.
    • $33
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  • Pyrimethamine
    T084958-14-0
    Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
    • $38
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  • Sulfameter
    T0748651-06-9
    Sulfameter (Sulfametoxydiazine) is a long-acting sulfonamide antibacterial agent used to treat urinary tract infections and leprosy.
    • $30
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  • Pelitrexol
    T14147446022-33-9
    Pelitrexol (AG 2037) is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor.
    • $521
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  • LY 345899
    T1582710538-99-5
    LY 345899 is a Folate analog and is a methylenetetrahydrofolate dehydrogenase and MTHFD2 inhibitor (IC50: 96 nM and 663 nM, respectively and a Ki: 18 nM for MTHFD1).
    • $152
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    TargetMol | Citations Cited
  • Brodimoprim
    T1985856518-41-3
    Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR). Brodimoprim is also a long-acting broad-spectrum antibacterial agent characterized by a good pharmacokinetic profile.
    • $49
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  • Sulfadoxine
    T08362447-57-6
    Sulfadoxine (Sulphadoxine) is a broad-spectrum sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with bacteriostatic and antimalarial properties.
    • $41
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  • Pemetrexed disodium
    T0189L150399-23-8
    Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.
    • $37
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  • DS18561882
    T111032227149-22-4
    DS18561882 is an orally available, selective and potent inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) with antitumor activity, inhibits MTHFD1 activity and can be used in the study of breast cancer.
    • $132
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  • DS44960156
    T376552361327-08-2
    DS44960156 is a novel selective inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) that inhibits both MTHFD2 and MTHFD1 and can be used in cancer research.
    • $77
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  • (Rac)-Managlinat dialanetil
    T16009347870-26-2
    (Rac)-Managlinat dialanetil ((Rac)-MB06322) is the racemate of Managlinat dialanetil, an orally available and potent inhibitor of fructose 1,6-bisphosphatase (FBPase) used in research 2 type diabetes.
    • $1,970
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  • LY 222306
    T11921154446-98-7
    LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
    • $1,670
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  • WR99210
    T1725747326-86-3
    WR99210 is a potent, orally available and less toxic dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 has good antiparasitic activity against P. vivax and P. falciparum strains (including P. falciparum strains resistant to Pyrimethamine ) and T. gondii.
    • $108
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