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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).
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T17257 WR99210 47326-86-3 98%
WR99210
WR99210 is a potent, orally available and less toxic dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 has good antiparasitic activity against P....
T0189L Pemetrexed disodium 150399-23-8 99.92%
Pemetrexed disodium
Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer an...
T1153 Trimethoprim 738-70-5 99.81%
Trimethoprim
Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor...
T8003 Methotrexate disodium 7413-34-5 99.77%
Methotrexate disodium
Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor
T0849 Pyrimethamine 58-14-0 99.74%
Pyrimethamine
Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
T24403 Folinic acid 58-05-9 99.7%
Folinic acid
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-induce...
T1485 Methotrexate 59-05-2 99.46%
Methotrexate
Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive act...
T0148 Folinic acid calcium 1492-18-8 99.3%
Folinic acid calcium
Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.
T2204 Diaveridine 5355-16-8 99.19%
Diaveridine
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 m...
T6226 Pemetrexed disodium hemipenta hydrate 357166-30-4 99.16%
Pemetrexed disodium hemipenta hydrate
Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Diso...
T8548 Metoprine 7761-45-7 99.09%
Metoprine
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
T6120 Pralatrexate 146464-95-1 98.56%
Pralatrexate
Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carr...
T6431 Levoleucovorin Calcium 80433-71-2 98.46%
Levoleucovorin Calcium
Levoleucovorin Calcium (CL307782), a calcium salt of the folinic acid, is used in cancer chemotherapy as an adjuvant.
T4382 Proguanil hydrochloride 637-32-1 98.13%
Proguanil hydrochloride
Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguani...
T7730 Aminopterin 54-62-6 98%
Aminopterin
Aminopterin (4-Aminofolic acid) is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase
T7593 Levomefolate calcium 151533-22-1 98%
Levomefolate calcium
Levomefolate calcium is an artificial form of folate. It is a coenzymated form of folic acid and a more bioavailable alternative in dietary supplements.
T16045 Methotrexate metabolite 19741-14-1 95.28%
Methotrexate metabolite
Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherape...
T0148L Folinic Acid Calcium Salt Pentahydrate 6035-45-6 100%
Folinic Acid Calcium Salt Pentahydrate
Folinic Acid Calcium Salt Pentahydrate (Leucovorin Calcium Pentahydrate), a reduced folic acid, is used in combination with other chemotherapeutics.
T0189 Pemetrexed 137281-23-3 100%
Pemetrexed
Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
T7598 Calcium N5-methyltetrahydrofolate 26560-38-3
Calcium N5-methyltetrahydrofolate
Calcium N5-methyltetrahydrofolate (NSC-173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advan...
WR99210
T17257
WR99210 is a potent, orally available and less toxic dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 has good antiparasitic activity against P....
Pemetrexed disodium
T0189L
Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer an...
Trimethoprim
T1153
Trimethoprim (NSC-106568) is a Dihydrofolate Reductase Inhibitor Antibacterial. The mechanism of action of trimethoprim is as a Dihydrofolate Reductase Inhibitor...
Methotrexate disodium
T8003
Methotrexate disodium is an tetrahydrofolate dehydrogenase inhibitor
Pyrimethamine
T0849
Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.
Folinic acid
T24403
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-induce...
Methotrexate
T1485
Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive act...
Folinic acid calcium
T0148
Folinic acid calcium (Leucovorin Calcium) is the active metabolite of folic acid. Leucovorin is used principally as an antidote to folic acid antagonists.
Diaveridine
T2204
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 m...
Pemetrexed disodium hemipenta hydrate
T6226
Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Diso...
Metoprine
T8548
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
Pralatrexate
T6120
Pralatrexate (10-Propargyl-10-deazaaminopterin) is a folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carr...
Levoleucovorin Calcium
T6431
Levoleucovorin Calcium (CL307782), a calcium salt of the folinic acid, is used in cancer chemotherapy as an adjuvant.
Proguanil hydrochloride
T4382
Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguani...
Aminopterin
T7730
Aminopterin (4-Aminofolic acid) is a synthetic folic acid derivative whose metabolite is a competitive inhibitor of dihydrofolate reductase
Levomefolate calcium
T7593
Levomefolate calcium is an artificial form of folate. It is a coenzymated form of folic acid and a more bioavailable alternative in dietary supplements.
Methotrexate metabolite
T16045
Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherape...
Folinic Acid Calcium Salt Pentahydrate
T0148L
Folinic Acid Calcium Salt Pentahydrate (Leucovorin Calcium Pentahydrate), a reduced folic acid, is used in combination with other chemotherapeutics.
Pemetrexed
T0189
Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).
Calcium N5-methyltetrahydrofolate
T7598
Calcium N5-methyltetrahydrofolate (NSC-173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advan...
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TargetMol