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DHFR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Translational Lung Cancer Research, April 2022, 543-559
iScience, 2024, 27(10):110862
Cell Rep, 2022, 38(9):110448
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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
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S1236 Leucovorin Calcium Pentahydrate (Folinic acid) Leucovorin (Folinic acid) Calcium Pentahydrate is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition.Solutions are unstable and should be fresh-prepared.
Journal of Hepatocellular Carcinoma, March 27, 2023, 483-495
Journal of Student Research, August 2024, nan
J Exp Clin Cancer Res, 2025, 44(1):13
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
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
Drug Resistance Updates, 2023, 101005
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.
Int J Med Sci, 2022 Jan 1, 233-241
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.
Molecular Cancer Research, January 02, 2024, 82-93
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).
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.
S5136 Calcium folinate (Leucovorin calcium) Calcium folinate (Leucovorin calcium) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives.Solutions are unstable and should be fresh-prepared.
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.
Cancer Res, 2026, 86(7):1724-1738
J Clin Invest, 2025, e190215
Theranostics, 2025, 15(10):4526-4549
Verified customer review of Methotrexate
S1135 Pemetrexed Disodium (LY231514) Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Frontiers in Pharmacology, September 27, 2021, 718675
Cancer Research, November 2, 2022, 4079-4092
Frontiers in Oncology, August 18, 2021, 711043
Verified customer review of Pemetrexed Disodium (LY231514)
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.
Anticancer Research, 2026, 1323-1335
Nat Commun, 2025, 16(1):7853
Nat Commun, 2025, 16(1):8476
S3129 Trimethoprim Trimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections.
Cell Rep, 2024, 43(7):114500
Sci Rep, 2024, 14(1):9167
CHALMERS UNIVERSITY OF TECHNOLOGY, 2023,
S5927 Proguanil Proguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication.
Int J Med Sci, 2022, 233-241
International Journal of Medical Sciences, 2022, 233-241
International Journal of Medical Sciences, 2022, 19(2):233-241