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Antifolate Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1210 Methotrexate Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
J Clin Invest, 2025, e190215
Theranostics, 2025, 15(10):4526-4549
Antimicrob Agents Chemother, 2025, e0047125.
Verified customer review of Methotrexate
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. This compound stimulates autophagy and apoptosis.
iScience, 2024, 27(10):110862
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
Verified customer review of Pemetrexed Disodium Hydrate
S5971 Pemetrexed Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. This compound induces autophagy and apoptosis.
Nat Commun, 2025, 16(1):7853
Nat Commun, 2025, 16(1):8476
Sci Adv, 2025, 11(4):eadp4765
S5097 Methotrexate disodium Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.
Chin Med J (Engl), 2023, 10.1097/CM9.0000000000002816
Pharmaceutics, 2023, 15(2)576
Bioact Mater, 2022, 18:459-470
S1497 Pralatrexate Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. This compound induces tumor cell apoptosis.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Br J Haematol, 2024, 10.1111/bjh.19658
Discov Oncol, 2024, 15(1):709
Verified customer review of Pralatrexate
S2006 Pyrimethamine Pyrimethamine(RP 4753) is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug.
Antimicrob Agents Chemother, 2025, e0047125.
Int J Parasitol Drugs Drug Resist, 2025, 29:100626
BMC Cancer, 2024, 24(1):116
S5790 Folinic acid (Leucovorin) Folinic acid (Leucovorin) is a biological folic acid that increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase (TS).Solutions are unstable and should be fresh-prepared.
Nat Cell Biol, 2024,
Nat Commun, 2022, 13(1):6308
S2588 Calcium Folinate Calcium Folinate is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy.Solutions are unstable and should be fresh-prepared.
Drug Resist Updat, 2023, 71:101005
E1003 Aminopterin Aminopterin (4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739), a folic acid antagonist, is a competitive inhibitor of dihydrofolate reductase (DHFR) with Ki of 3.7 pM.
Mol Cancer Res, 2024, 22(1):82-93
E4837 Trimethoprim (lactate) Trimethoprim (lactate) is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), an essential enzyme responsible for the production of tetrahydrofolic acid (THF). By blocking this enzyme, it prevents the synthesis of bacterial DNA, hindering bacterial survival. This compound is a standard antibiotic for treating urinary tract infections (UTIs).
S3082 Proguanil HCl(Atovaquone) Proguanil hydrochloride (Chloroguanil, Chlorguanide hydrochloride), also known as Atovaquone, is an antimalarial proagent that acts as an inhibitor of dihydrofolate reductase (DHFR). It functions as a biguanide to enhance the effect of Atovaquone.
S5200 Diaveridine Diaveridine (AI3-23935, CCRIS-3784) is a coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis.