1-(4-Chlorophenyl)biguanide is a guanide derivative that can inhibit dihydrofolate reductase (DHFR).

Folinic acid is a reduced folic acid, which is used in combination with other chemotherapy drugs.

Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.

Calcium levofolinate is the calcium salt of levoleucovorin, which is the enantiomerically active form of folinic acid.

Proguanil is an inhibitor of dihydrofolate reductase (DHFR). It is antimalarial prodrug metabolized to the active metabolite cycloguanil.

Levomefolate Calcium is an artificial form of folate.

Pemetrexed disodium is an antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Levomefolic acid is the natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions.

Pemetrexed disodium is a guanine-derived antineoplastic agent that functions as a nucleic acid synthesis inhibitor through its binding to, and inhibition of, thymidylate synthase.

Leucovorin calcium is a reduced form of folic acid.

Pyrimethamine inhibits multidrug and toxin extrusion (MATE) transporter potently, it also inhibits dihydrofolate reductase (DHFR), used for protozoal infections and interferes with tetrahydrofolic acid synthesis from folic acid. Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways.

Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with Ki of 11.5 nM, also an antibacterial agent.

Trimethoprim is a synthetic antibiotic that inhibits dihydrofolate reductase (DHFR) which is necessary for the synthesis of purines, amino acids, and thymidylic acid, with prominent selectivity for bacterial DHFR over mammalian DHFR (IC50s = 5 and 30,000 nM, respectively). Trimethoprim is used mainly in the prophylaxis and treatment of urinary tract infections.

Methotrexate, an antifolate compound, 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 and can interfere with the growth of certain cells of the body, especially cells that reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.

Cycloguanil HCl is HCl form of cycloguanil which is a metabolite of proguanil and a dihydrofolate reductase inhibitor.

Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.