Catalog No.
Product Name
Application
Product Information
Citations
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DHFR inhibitor
Methotrexate is a cytotoxic agent that inhibits thymidylate synthetase and de novo purine synthesis. -
DHFR inhibitor
NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. -
DHFR inhibitor
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.- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
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DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. - Aminopterin is an antineoplastic drug. It works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase.
- Nobuo Aikawa, .et al. , J Toxicol Sci, 2020, 45(4):187-199 PMID: 32238694
- Trimetrexate is a quinazoline derivative. It is a dihydrofolate reductase inhibitor.
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DHFR inhibitor
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. -
DHFR inhibitor
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. -
DHFR Inhibitor
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. -
VEGFR-2/DHFR Inhibitor
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. -
DHFR Inhibitor
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 Inhibitor
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. -
EGFR/HER2/DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
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. -
DHFR Inhibitor
Fluorofolin is a potent dihydrofolate reductase (DHFR) inhibitor, demonstrating an IC50 of 2.5 nM. This compound exhibits significant antimicrobial activity against Pseudomonas aeruginosa, making it a valuable reagent for research in antibacterial drug development and mechanisms of resistance. Fluorofolin is suitable for studies involving folate metabolism and has potential applications in exploring therapeutic strategies targeting DHFR-related pathways. -
DHFR Inhibitor
Phomarin is a specific inhibitor of dihydrofolate reductase (DHFR), an enzyme critical for folate metabolism. It demonstrates potential antimalarial activity, making it a valuable tool for research in malaria treatment and prevention. Its mechanism of action supports further investigations into antifolate strategies and their implications for drug development. -
DHFR Inhibitor
DHFR-IN-5 is a highly potent and orally bioavailable inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against the quadruple mutant strain of Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research into malaria therapeutics and the study of resistance mechanisms in Plasmodium species. -
DHFR Substrate
10-Formyl-7,8-dihydrofolic acid is a potent substrate for dihydrofolate reductase (DHFR) and aminoimidazolecarboxamide ribonucleotide transformylase. It plays a significant role in promoting the growth of leukemia cells and can effectively reverse growth inhibition caused by antifolate medications in folate-deficient environments. This compound is valuable for research applications focused on leukemia and related therapeutic strategies. -
DHFR Inhibitor
Epiroprim is a selective inhibitor of dihydrofolate reductase (DHFR), a key enzyme in folate metabolism. It exhibits potent antibacterial activity against various Gram-positive bacterial strains, including staphylococci, enterococci, pneumococci, and streptococci. Epiroprim is commonly utilized in research applications focused on antimicrobial resistance and drug development strategies targeting bacterial infections. -
Dihydrofolate reductase (DHFR)
Piritrexim isethionate is a fat-soluble inhibitor of dihydrofolate reductase (DHFR), primarily used in the treatment of severe psoriasis. This compound exhibits comparable efficacy to methotrexate for psoriasis management, while potentially offering a reduced risk of hepatotoxicity. Its selective target and biological activity make it a valuable reagent for research focusing on autoimmune skin disorders and folate metabolism. -
DHFR Inhibitor
Methotrexate diethyl ester is a potent inhibitor of dihydrofolate reductase (DHFR). This compound demonstrates significant biological activity in the context of T. cruzi infection and leukemia research, making it valuable for investigating therapeutic strategies in these disease areas. Its ability to inhibit DHFR underscores its potential applications in studies focusing on cancer and parasitic infections. -
Dihydrofolate reductase (DHFR)
Zymosterone is a biochemical reagent that targets dihydrofolate reductase (DHFR). It is converted into zymosterol, an essential intermediate in cholesterol biosynthesis, through the action of hydroxysteroid (17β) dehydrogenase 7 (HSD17B7). This transformation, further catalyzed by 3-keto sterol reductase (ERG27), is critical for the biosynthesis of ergosterol in yeast, facilitating studies in lipid metabolism and cellular function. -
DHFR-TS PROTAC Degrader
BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival. -
DHFR Inhibitor
DHFR-IN-9 is a potent inhibitor of dihydrofolate reductase (DHFR), critically involved in purine and thymidylate biosynthesis, playing a significant role in cellular proliferation and growth. This compound demonstrates robust antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 0.25 μg/mL, as well as notable anti-infective effects in mouse models of systemic and thigh infections. Additionally, DHFR-IN-9 exhibits superior anticancer efficacy compared to paclitaxel in a mouse breast cancer model, administered at 2.5 mg/kg every three days. -
DHFR Inhibitor
DHFR-IN-8 is a potent dihydrofolate reductase (DHFR) inhibitor that disrupts purine and thymidylate biosynthesis, thereby impeding cell proliferation and growth. This compound exhibits significant antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300, with an IC50 value of 15.6 ng/mL. DHFR-IN-8 is applicable in research focused on tackling systemic infections and thigh infections in murine models. -
DHFR Inhibitor
DHFR-IN-22 is a potent inhibitor of Dihydrofolate Reductase (DHFR), classified as a 2,4-diaminopyrimidine compound. It demonstrates remarkable inhibitory activity against purified DHFR and key non-tuberculous mycobacterial species, including Mycobacterium avium and Mycobacterium abscessus, with IC50 values of 1.1 nM and 6.3 nM, respectively, and MIC values of 1.5 μg/mL and 0.1 μg/mL, respectively. In contrast, it exhibits a significantly higher IC50 of 2100 nM against human DHFR. DHFR-IN-22 is valuable for investigating therapeutic strategies to address NTM infections. -
DHFR Inhibitor
10-Deazaaminopterin is a potent inhibitor of dihydrofolate reductase (DHFR), an essential enzyme involved in folate metabolism. This compound has demonstrated significant anti-tumor activity and is primarily utilized in cancer research to investigate its effects on cellular proliferation and metabolism. Its application is particularly relevant in studies focusing on advanced cancer therapies and folate-dependent biochemical pathways. -
PROTAC DHFR Degrader
PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum. -
DHFR Inhibitor
DHFR-IN-24 is a dihydrofolate reductase (DHFR) inhibitor with a benzothiazole structure. This compound exhibits intrinsic antibacterial activity against Gram-positive and Gram-negative bacteria. Additionally, it demonstrates a synergistic effect when combined with photodynamic therapy (PDT), enhancing antibacterial efficacy against multidrug-resistant pathogens. Research applications include studying bacterial resistance mechanisms and developing novel antibacterial therapies. -
DHFR Inhibitor
DHFR-IN-5 hydrochloride is a potent inhibitor of dihydrofolate reductase (DHFR), exhibiting a Ki value of 0.54 nM against quadruple mutant Plasmodium falciparum DHFR. This compound demonstrates significant anti-malarial activity, making it a valuable tool for research in malaria treatment and drug development targeting DHFR pathways. -
DHFR Inhibitor
DHFR-IN-19 is a selective inhibitor of dihydrofolate reductase (DHFR) specifically targeting Trypanosoma brucei. With a Ki value of 9 nM, DHFR-IN-19 demonstrates significant antiparasitic activity, exhibiting an EC50 of 14.5 μM. This compound serves as a valuable tool for research into treatments for diseases caused by Trypanosoma brucei, particularly in the context of potential therapeutic applications against African sleeping sickness. -
DHFR Inhibitor
DDPO is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 of 0.035 µM. This compound demonstrates significant anticancer activity by inhibiting the growth of L1210 and WI-L2 cell lines, with IC50 values of 5 µM and 0.28 µM, respectively. DDPO is primarily used in research applications focusing on cancer therapeutics and DHFR-related pathways. -
DHFR/TS Inhibitor
CB 3705 is a potent inhibitor of dihydrofolate reductase (DHFR) and thymidylate synthetase (TS). This compound demonstrates significant anti-cancer activity, exhibiting ID50 values of 4.77 μM against L1210 cells and 408 μM against the mutant L1210:C15 cell line. Its inhibition of key enzymes involved in nucleotide synthesis makes CB 3705 a valuable tool for cancer research and drug development. -
DHFR Inhibitor
Aditoprime is a selective inhibitor of bacterial dihydrofolate reductase (DHFR), demonstrating IC50 values of 47 nM and 520 nM for E. coli and L. casei DHFR, respectively. By inhibiting the conversion of dihydrofolic acid to tetrahydrofolic acid, Aditoprime effectively impairs bacterial folate synthesis. This compound exhibits broad-spectrum antibacterial activity and possesses favorable pharmacokinetic properties, making it a useful reagent in microbiological research and antibiotic development studies. -
DHFR Inhibitor
Tetroxoprim is a potent dihydrofolate reductase (DHFR) inhibitor with significant antimicrobial properties. It serves as a critical tool in the study of antimicrobial resistance and the development of new therapeutic agents. Its ability to inhibit folate synthesis makes it valuable for research in infectious disease and related biochemical pathways. -
DHFR Inhibitor
Fanotaprim is a selective inhibitor of dihydrofolate reductase (DHFR), demonstrating IC50 values of 1.57 nM for Toxoplasma gondii DHFR and 308 nM for human DHFR. This compound is particularly relevant for investigating toxoplasmosis, providing insight into potential therapeutic strategies against this parasitic infection. Its targeted inhibition of tgDHFR makes Fanotaprim a valuable tool for research in pharmacology and microbiology. -
Folic Acid/DHFR Antagonist
Aminopterin sodium is a folic acid antagonist that primarily targets dihydrofolate reductase (DHFR). By inhibiting DHFR, it disrupts folate metabolism, leading to decreased nucleic acid synthesis. This compound is primarily utilized in the treatment of acute lymphoblastic leukemia and various cancers. Additionally, Aminopterin sodium is employed as an immunosuppressant for the management of autoimmune disorders. -
DHFR Inhibitor
Lysine-methotrexate is a dihydrofolate reductase (DHFR) inhibitor, structurally related to Methotrexate. This compound exhibits potent biological activity by inhibiting folate metabolism, making it useful in studying cellular processes that rely on nucleotide synthesis. Lysine-methotrexate is applicable in cancer research and other therapeutic contexts where modulation of DHFR activity is of interest. -
MtDHFR Inhibitor
DHFR-IN-2 is a potent uncompetitive inhibitor of MtDHFR (dihydrofolate reductase from Mycobacterium tuberculosis), demonstrating an IC50 value of 7 μM. This compound serves as a valuable tool for tuberculosis research, aiding in the study of pathogenic processes and potential therapeutic strategies against TB. -
DHFR Inhibitor
Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an established antifolate agent. This compound functions as an antimetabolite, exhibiting cytotoxic effects on rapidly dividing cells, making it relevant for cancer research. Its ability to inhibit DHFR provides a valuable tool for investigating folate metabolism and developing therapeutic strategies against various malignancies. -
DHFR Inhibitor
TNP-351 is a dihydrofolate reductase (DHFR) inhibitor known for its potent antitumor activity. This antifolate compound exhibits efficacy against both leukemia and solid tumor cells in vitro and in vivo, making it a valuable tool in cancer research. Its mechanism of action involves the disruption of folate metabolism, ultimately hindering DNA synthesis and cell proliferation. -
DHFR Inhibitor
DHFR-IN-3 is a dihydrofolate reductase (DHFR) inhibitor that demonstrates an IC50 of 19 μM in rat liver DHFR and 12 μM in P. carinii DHFR. This compound is primarily utilized in pharmacological research to study the role of DHFR in folate metabolism and its implications in various disease states, including cancer and parasitic infections. Its inhibitory activity makes it a valuable tool for investigating potential therapeutic strategies targeting DHFR-related pathways.
