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Antifolate

Antifolates are a class of antimetabolite medications that antagonise (that is, block) the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. 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. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR).

  • Methotrexate
    T148559-05-2
    Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.
    • $38
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    TargetMol | Citations Cited
  • 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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  • Folinic acid calcium
    T01481492-18-8
    Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.
    • $42
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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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  • Proguanil hydrochloride
    T4382637-32-1
    Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite.
    • $50
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  • Methotrexate metabolite
    T1604519741-14-1In house
    Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.
    • $39
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    TargetMol | Inhibitor Sale
  • 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
  • Calcium N5-methyltetrahydrofolate
    T759826560-38-3
    Calcium N5-methyltetrahydrofolate (NSC-173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers
    • $76
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    TargetMol | Inhibitor Sale
  • Farletuzumab
    T76720896723-44-7
    Farletuzumab (MORAb-003) is a potent inhibitor of folate receptor-α (FRα). Farletuzumab is a humanized monoclonal antibody with a high affinity for FRα. Farletuzumab inhibits the growth of cells that overexpress FRα. Farletuzumab can be used to study cancer.
    • $372
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    TargetMol | Inhibitor Sale
  • Levoleucovorin Calcium
    T643180433-71-2
    Levoleucovorin Calcium (CL307782), a calcium salt of the folinic acid, is used in cancer chemotherapy as an adjuvant.
    • $36
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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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  • Mirvetuximab
    T767661453084-36-0
    Mirvetuximab (M9346A) is a novel folate receptor α (FRα) monoclonal antibody targeting anti-FOLR1 (folate receptor 1). Mirvetuximab soravtansine is often conjugated with platinum compounds or other compounds to form antibody-drug conjugates for the treatment of ovarian cancer and other FRα-positive cancers.
    • $322
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    TargetMol | Inhibitor Sale
  • 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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  • Pyrimethamine
    T084958-14-0
    Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
    • $38
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  • Folinic Acid Calcium Salt Pentahydrate
    T0148L6035-45-6
    Folinic Acid Calcium Salt Pentahydrate (Leucovorin Calcium Pentahydrate), a reduced folic acid, is used in combination with other chemotherapeutics.
    • $41
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  • Folinic acid
    T2440358-05-9
    Folinic acid (Leucovorin) is a biofolic acid that can be used in the treatment of methotrexate, often in combination with Methotrexate (MTX) to reduce MTX-induced toxicity, and can be used as an adjuvant treatment for colon cancer.
    • $33
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  • Methotrexate disodium
    T80037413-34-5
    Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor
    • $34
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  • Metoprine
    T85487761-45-7
    Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
    • $55
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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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  • Levomefolate calcium
    T7593151533-22-1
    Levomefolate calcium is an artificial form of folate. It is a coenzymated form of folic acid and a more bioavailable alternative in dietary supplements.
    • $39
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  • Aminopterin
    T773054-62-6
    Aminopterin (4-Aminofolic acid) is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase
    • $41
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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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