Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Endogenous Metabolite
DL-Norvaline is a derivative of L-norvaline that serves as a non-competitive inhibitor of arginase. By inhibiting this enzyme, DL-Norvaline can influence the L-arginine metabolism pathway, affecting nitric oxide production and supporting various biological processes. It is utilized in research applications focused on metabolic pathways, nitric oxide synthesis, and related physiological effects. -
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. -
AhR Agonist
MeBIO is a potent aryl hydrocarbon receptor (AhR) agonist, exhibiting an IC50 of 44 μM for GSK-3 and 55 μM for CDK1/cyclin B interactions. This compound is primarily utilized in research to explore the role of AhR signaling in various biological processes, such as immune response regulation and cellular differentiation. Researchers can employ MeBIO to investigate its effects in toxicology studies and the development of therapeutic strategies targeting AhR pathways. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
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. -
SCDKI Pathway Inhibitor
SNX7 is a selective inhibitor of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. This compound plays a crucial role in studying cellular senescence and various CDKI-related diseases. By targeting the CDKI pathway, SNX7 serves as a valuable tool in cancer research and other conditions where cell cycle regulation is disrupted. -
Alkyltriazine Herbicide
Indaziflam is an alkyltriazine herbicide that acts by targeting the cellulose synthase complex, leading to the inhibition of cellulose biosynthesis in plant cell walls. This compound induces notable physiological alterations in plants, including radial swelling, ectopic lignification, and abnormal root and cell morphology, as well as reduced root and hypocotyl elongation. Additionally, Indaziflam has been shown to cause DNA strand breaks and micronucleus formation in HepG2 cells, making it a valuable reagent for research on monocot weed control and understanding herbicide mechanisms. -
Cathepsin L Inhibitor
Gallinamide A is a potent inhibitor of cathepsin L, demonstrating an IC50 value of 17.6 pM. This compound plays a crucial role in research applications focused on investigating the functions of cathepsin L in various biological processes, including protein degradation and immune response regulation. Its inhibitory activity makes Gallinamide A a valuable tool for studying the implications of cathepsin L in pathophysiological conditions. -
RAR Agonist
MDI-403 is a highly potent retinoic acid receptor (RAR) agonist, exhibiting an EC50 value of less than 1 μM. It demonstrates significant antiviral activity against SARS-CoV-2 by dose-dependently inhibiting the expression of viral nucleoprotein (NP) and decreasing the proportion of infected cells, mainly during the virus invasion stage. MDI-403 serves as a valuable tool for research focused on the mechanisms of antiviral activity and potential therapies against SARS-CoV-2. -
α-Glucosidase Inhibitor
DNJ-20 is an α-glucosidase inhibitor with an IC50 of 55.3 μg/mL, demonstrating significant broad-spectrum activity against SARS-CoV-2. It disrupts the endoplasmic reticulum-associated glycoprotein folding process, inhibiting proper processing of viral glycoproteins and consequently blocking viral particle formation and infection. DNJ-20 exhibits IC50 values as low as 1.49 μM against various SARS-CoV-2 variants, as well as HCoV-229E and HCoV-OC43. This inhibitor is suited for pan-coronavirus research applications. -
CYP2C1/CYP2C19 Inhibitor
CYP2C1/CYP2C19-IN-2 is a potent inhibitor of the CYP2C1 and CYP2C19 enzymes. This compound exhibits minimal hepatotoxicity and lacks Ames toxicity, making it a safer choice for research applications. CYP2C1/CYP2C19-IN-2 is particularly useful in studies investigating antiviral mechanisms against Zika virus (ZIKV). -
CYP2C9/CYP2C19 Inhibitor
CYP2C9/CYP2C19-IN-1 is a potent inhibitor of the cytochrome P450 enzymes CYP2C9 and CYP2C19. This compound exhibits key biological activity by effectively modulating drug metabolism pathways without hepatotoxic effects or Ames toxicity. It serves as a valuable tool for research applications, including studies on anti-Zika virus (ZIKV) therapeutics. -
MAO-A/B Inhibitor
Tedizolid phosphate sodium is a selective inhibitor of monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). This compound exhibits significant activity against Gram-positive bacteria, making it valuable in the study of antimicrobial resistance and the development of new therapeutic agents. Its mechanisms of action and inhibition properties facilitate research into neurological disorders and other conditions associated with monoamine dysregulation. -
Endogenous Metabolite
Farnesol is a sesquiterpene alcohol that functions as an endogenous metabolite with notable antimicrobial properties. It has been shown to modulate cell-to-cell communication in Candida albicans and exhibits inhibitory activity against various bacterial species. This compound is valuable for research in microbial interactions and the modulation of pathogenic behaviors. -
α-glucosidase Inhibitor
1-Deoxynojirimycin hydrochloride is a potent α-glucosidase inhibitor, primarily utilized for modulating postprandial blood glucose levels. This compound demonstrates notable antihyperglycemic and anti-obesity effects, making it valuable in diabetes mellitus research. Additionally, 1-Deoxynojirimycin hydrochloride exhibits antiviral properties, contributing to its diverse applicability in metabolic and infectious disease studies. -
HMG-CoA Synthase Inhibitor
Hymeglusin is a fungal β-lactone antibiotic that functions as a potent inhibitor of HMG-CoA synthase, exhibiting an IC50 of 0.12 μM. This compound covalently modifies the active cysteine residue at position 129 of the enzyme, thereby disrupting its activity. Hymeglusin is primarily utilized in research applications focused on lipid metabolism and studying the modulation of cholesterol biosynthesis pathways. -
Phospholipase C Inhibitor, Angiogenesis Modulator
Neomycin is an aminoglycoside antibiotic known for its role as a phospholipase C (PLC) inhibitor and angiogenesis modulator. It effectively inhibits the nuclear translocation of angiogenin, resulting in reduced cell proliferation and angiogenesis. Additionally, Neomycin interferes with IP3-mediated calcium release and MgATP-dependent calcium uptake, influencing skeletal muscle calcium transients. Its ability to modulate crucial biological pathways makes Neomycin a valuable tool for cancer research and understanding microbial impact on health. Prolonged exposure may lead to adverse effects such as hearing impairment and kidney damage. -
Cytochrome P450 Inhibitor
Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections. -
Fungal Metabolite
Colletodiol is a fungal metabolite that demonstrates immunosuppressant and antiviral activities. This compound effectively inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes, with IC50 values of 12 and 5 μg/mL, respectively. Additionally, Colletodiol has been shown to inhibit influenza A viral replication in HeLa-IAV-Luc cells, making it a valuable tool for research in immunology and virology. -
MAO Inhibitor
Eckol is a potent inhibitor of human monoamine oxidase A (hMAO-A) and a non-competitive inhibitor of human monoamine oxidase B (hMAO-B), with IC50 values of 7.20 μM and 83.44 μM, respectively. This compound exhibits significant biological activity through its antiallergic and antiviral effects, making it a valuable tool for exploring these pathways. Additionally, Eckol promotes stimulatory effects in maize and may serve as an effective plant biostimulant in agricultural research applications. -
CYP51 Inhibitor
Obtusifoliol is a selective inhibitor of cytochrome P450 51 (CYP51), demonstrating affinities with dissociation constants (Kd) of 1.2 μM for Trypanosoma brucei and 1.4 μM for human CYP51. This compound is significant in studies focused on trypanosomiasis, targeting the sterol biosynthesis pathway. Its inhibition of CYP51 may provide valuable insights into therapeutic strategies against related infections and contribute to the understanding of cholesterol metabolism in various biological systems. -
ChE Inhibitor
N-p-trans-Coumaroyltyramine is a natural phenolic amide compound that acts as an inhibitor of acetylcholinesterase (AChE) with an IC50 of 122 μM and α-glucosidase with an IC50 of 2.7 μM. It demonstrates significant anti-trypanosomal activity, exhibiting an IC50 of 13.3 µM against Trypanosoma brucei rhodesiense. This compound is valuable for research into neurodegenerative diseases such as Alzheimer's disease, as well as for studies focusing on trypanosomiasis. -
Endogenous Metabolite
L-Canaline is a nonprotein amino acid primarily associated with leguminous plants. It acts as a potent and irreversible inhibitor of ornithine aminotransferase and exhibits cytotoxic properties. L-Canaline has demonstrated significant antiproliferative effects and inhibits the growth of the malaria parasite Plasmodium falciparum, with an IC50 value of 297 nM. This compound is valuable for research applications in cancer biology and metabolic studies involving endogenous metabolites. -
Endogenous Metabolite
Tridecanedioic acid is an endogenous metabolite that plays a significant role in metabolic regulation, particularly in the context of non-alcoholic fatty liver disease (NASH). This compound serves as a potential node in the interaction network between intestinal microbiota and host metabolism. It is notably accumulated in resilient cabbage-type rapeseed varieties, indicating its involvement in plant defense mechanisms against pests such as the small cabbage moth (Plutella xylostella). Additionally, tridecanedioic acid may serve as a valuable biomarker for assessing plant insect resistance and diagnosing metabolic diseases.
