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Dihydrofolate reductase (DHFR) inhibitors block the enzyme that reduces dihydrofolate to tetrahydrofolate. Tetrahydrofolate carries one-carbon units for the synthesis of thymidylate, purines and several amino acids, so DHFR inhibition starves dividing cells of DNA precursors. In 1958 aminopterin and amethopterin, the compound now called methotrexate, were shown to inhibit the enzyme. Methotrexate, aminopterin and pralatrexate are classical antifolates, whereas the lipophilic trimetrexate enters cells without the folate carrier. Pemetrexed, described in 1997 as LY231514, also inhibits thymidylate synthase and glycinamide ribonucleotide formyltransferase. Proguanil, whose metabolite cycloguanil acts on the parasite enzyme, and the diaminopyrimidine diaveridine represent inhibitors of microbial DHFR.
Synonyms: LY-231514; Alimta
Pemetrexed disodium is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting three enzymes used in purine and pyrimidine synthesis–thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase.
Synonyms: 4-aminopteroic acid
Aminopterin is an antineoplastic drug. It works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase.
Synonyms: MTX; amethopterin; Rheumatrex; Trexall; Abitrexate
Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis.
Synonyms: Methotrexate metabolite; DAMPA
NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM.
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: CI-898
Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase 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: EGIS-5645
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
Proguanil is a potent dihydrofolate reductase (DHFR) inhibitor, primarily utilized in antimalarial research. Upon administration, it is metabolized to Cycloguanil, its active form, enhancing its efficacy against Plasmodium species. This compound is essential for studying the biochemical pathways of folate metabolism and developing therapeutic strategies against malaria.
WR99210 is a effective inhibitor of dihydrofolate reductase (DHFR) with an IC50 of
DHFR-IN-25 is a potent inhibitor of dihydrofolate reductase (DHFR), demonstrating broad-spectrum antibacterial activity. This compound exhibits significant efficacy against pathogens such as Candida albicans and Staphylococcus aureus. DHFR-IN-25 is particularly valuable for research applications focusing on local anti-infection strategies and the development of antimicrobial therapies.
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VEGFR-2/DHFR-IN-2 is a dual inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) and Dihydrofolate Reductase (DHFR), exhibiting IC50 values of 0.623 μM and 9.085 μM, respectively. This compound demonstrates significant cytotoxic activity against various cancer cell lines, including C26, HepG2, and MCF7, with IC50 values ranging from 3.59 to 8.38 μM. VEGFR-2/DHFR-IN-2 is pertinent for research applications focused on cancer therapeutics and targeted inhibition of tumor angiogenesis.
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DHFR-IN-1 is a selective inhibitor of dihydrofolate reductase (DHFR) with an IC50 of 40.71 nM. This compound demonstrates significant antibacterial activity against both gram-positive and gram-negative bacteria, as well as moderate antifungal properties. Additionally, DHFR-IN-1 exhibits a strong synergistic effect when combined with Levofloxacin, characterized by a fractional inhibitory concentration index (FIC) value of 0.249, making it a valuable candidate for further research in antimicrobial applications.
VEGFR-2/DHFR-IN-1 is a dual inhibitor of VEGFR-2 and dihydrofolate reductase (DHFR), exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. This compound demonstrates significant antibacterial activity against various strains, including Escherichia coli and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, VEGFR-2/DHFR-IN-1 shows potent cytotoxic effects on cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM. This reagent is applicable for research exploring cancer therapeutics and microbial resistance.
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EGFR/HER2/DHFR-IN-1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and dihydrofolate reductase (DHFR). This compound demonstrates potent antitumor efficacy, with IC50 values of 0.153 μM for EGFR, 0.108 μM for HER2, and 0.291 μM for DHFR. EGFR/HER2/DHFR-IN-1 effectively arrests the cell cycle at the G1/S phase and promotes apoptosis in MCF-7 breast cancer cells, making it a valuable reagent for cancer research and therapeutic development.
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DHFR-IN-4 is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 value of 123 nM. In addition to its primary activity, DHFR-IN-4 exhibits inhibitory effects on epidermal growth factor receptor (EGFR) and HER2, with IC50 values of 246 nM and 357 nM, respectively. This compound demonstrates significant cytotoxic potency across a broad spectrum of cancer cell lines, making it a valuable tool for cancer research and drug development.
Synonyms: Chlorguanide triazine
Cycloguanil is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an IC50 of 10.8 μM against human DHFR. By disrupting the folate metabolic pathway, Cycloguanil impairs nucleotide synthesis and DNA replication, highlighting its role in malaria research through its inhibition of DHFR in Plasmodium. Additionally, it exhibits anticancer properties by inhibiting DHFR in human cancer cells and blocking the transcriptional activity of STAT3.
Synonyms: CI-898 isethionate
Trimetrexate isethionate is a potent dihydrofolate reductase (DHFR) inhibitor, effectively reducing DNA and RNA precursor synthesis, which leads to cytotoxicity. With IC50 values of 4.74 nM for human DHFR and 1.35 nM for Toxoplasma gondii DHFR, it demonstrates significant antimicrobial and antitumor activity. This compound is valuable for research applications targeting Pneumocystis carinii pneumonia (PCP) and various cancer types.
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Synonyms: CI-898 trihydrochloride
Trimetrexate trihydrochloride is a potent dihydrofolate reductase (DHFR) inhibitor that effectively reduces the synthesis of DNA and RNA precursors, leading to cell death. With IC50 values of 4.74 nM for human DHFR and 1.35 nM for Toxoplasma gondii DHFR, this compound demonstrates strong inhibitory activity. Trimetrexate trihydrochloride is utilized in research focused on Pneumocystis carinii pneumonia (PCP) and various cancer cell types, offering valuable insights into therapeutic applications.
4'-DTMP is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting Ki values of 5.1 nM for wild-type DHFR and 34.3 nM for the L28R variant. This compound features a polar modification that enhances local interactions with the enzyme, particularly affecting the hairpin structure of the M20 loop, which is crucial for internal communication within DHFR. Due to its inhibitory effects, 4'-DTMP may also have potential applications in targeting E. coli.
1954U89 is a potent, lipid-soluble inhibitor of dihydrofolate reductase (DHFR) with oral bioavailability. This compound demonstrates significant anticancer activity, making it a valuable tool in cancer research. Its ability to inhibit DHFR provides insights into folate metabolism and therapeutic strategies targeting rapidly proliferating cells.
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DAMPA methyl ester is a potent inhibitor of dihydrofolate reductase (DHFR), an enzyme critical for DNA synthesis and cell proliferation. This compound has significant implications in cancer research, particularly in the investigation of chemotherapy mechanisms. It serves as a valuable tool for studying the inhibition of folate metabolism and understanding its role in tumor growth and treatment resistance.
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Synonyms: BRL 6231
WR99210 hydrochloride is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 of less than 0.075 nM. This compound exhibits significant antiparasitic activity, demonstrating efficacy against Plasmodium falciparum strains and Toxoplasma gondii. WR99210 hydrochloride serves as a valuable tool in research focused on parasitic infections and the development of new therapeutic strategies targeting DHFR.
Synonyms: BW 301U; NSC 351521
Piritrexim is a potent dihydrofolate reductase (DHFR) inhibitor that demonstrates strong efficacy against Pneumocystis carinii and Toxoplasma gondii, with IC50 values of 0.038 and 0.011 μM, respectively. It has significant applications in AIDS research due to its ability to inhibit folate metabolism in pathogenic organisms. Additionally, Piritrexim exhibits anticancer properties, making it valuable for oncology research.
