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Antifolates are folic acid analogs that block the enzymes of folate-dependent nucleotide synthesis. Reduced folates carry one-carbon units for the synthesis of thymidylate and purines. Antifolates compete with these cofactors at dihydrofolate reductase (DHFR), thymidylate synthase (TS) or glycinamide ribonucleotide formyltransferase (GARFT). Depleted nucleotide pools then stall DNA replication in dividing cells. Methotrexate disodium and pralatrexate inhibit DHFR, while pemetrexed acts on DHFR, TS and GARFT. Nolatrexed Dihydrochloride is a lipophilic TS inhibitor, pelitrexol targets GARFT, and LSN 3213128 inhibits aminoimidazole carboxamide ribonucleotide formyltransferase (AICARFT). The set also includes reduced folates such as Levoleucovorin Calcium and Calcium N5-methyltetrahydrofolate, which supply folate in culture or bypass DHFR inhibition.
Synonyms: PDX; 10-Propargyl-10-deazaaminopterin; D05589
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.
Pemetrexed is a novel antifolate with multiple targets
Synonyms: AG 337; Thymitaq
Nolatrexed Dihydrochloride is an antifolate thymidylate synthase inhibitor.
Synonyms: Pemetrexed sodium hydrate (1:2:2.5)
Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
Synonyms: AG 2037
Pelitrexol is a GARFT inhibitor, and is also a water soluble antifolate with anti-proliferative activity.
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.
Synonyms: LY 09887
LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
AG2034 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), exhibiting a Ki value of 28 nM for human GARFT. It demonstrates high affinity for the folate receptor, with a Kd of 0.0042 nM, and serves as a substrate for rat liver folylpolyglutamate synthetase, exhibiting a Km of 6.4 µM. AG2034 effectively inhibits the proliferation of L1210 and CCRF-CEM cell lines, with IC50 values of 4 nM and 2.9 nM, respectively, and shows promising antitumor activity in xenograft models such as 6C3HED. This compound is suitable for research applications targeting GARFT-related pathways in cancer biology.
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5,10-Dideazafolic acid is a potent inhibitor targeting glycine amide ribonucleotide formyltransferase (GARFT), with an affinity characterized by a Ki value of 13 μM. This compound demonstrates significant inhibitory activity, making it a valuable tool for studying purine biosynthesis and related metabolic pathways. Its application extends to research on cancer metabolism and the development of potential therapeutic strategies targeting GARFT.
