Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-3 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum plays a critical role as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters necessary for Wnt activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the modulation of Wnt signaling pathways. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-2 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum functions as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters, which are essential for Wnt activity. This compound is valuable for investigating the role of Notum in cancer biology and the modulation of Wnt signaling pathways. -
Carboxylesterase Inhibitor
WZU-13 is a potent inhibitor of carboxylesterase (CES), demonstrating significant inhibition of 77% at a concentration of 100 μM. This compound is valuable for research applications aimed at studying the role of CES in drug metabolism and detoxification processes. WZU-13 can aid in elucidating the enzymatic mechanisms and biological functions of CES in various physiological and pathological contexts. -
SMO Inhibitor
IPI-269609 is a potent inhibitor of Smoothened (SMO), specifically targeting the Hedgehog (Hh) signaling pathway. This compound has demonstrated significant efficacy in reducing the ALDH-bright cell population, identified as cancer stem cells in pancreatic cancer. IPI-269609 effectively inhibits both the migration and colony formation of pancreatic cancer cells, and has shown effectiveness in mitigating pancreatic cancer metastasis in preclinical mouse models. Its application is invaluable for research focused on pancreatic cancer and the underlying mechanisms of tumor progression. -
5-LO/COX-2/DPP-4 Inhibitor
Timosaponin A1 is a natural steroidal saponin that acts as an inhibitor of 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2), and dipeptidyl peptidase 4 (DPP-4), with IC50 values of 3.29 µM, 36.43 µM, and 33.25 µM, respectively. This compound exhibits anti-inflammatory properties and is relevant for research on conditions such as asthma and diabetes. Its inhibitory effects on key enzymes involved in inflammatory pathways make it a valuable tool for exploring therapeutic strategies in related biological studies. -
Triterpenoid
Cyclocarin A is a triterpenoid compound isolated from the leaves of Cyclocarya paliurus. This compound exhibits weak inhibitory activity against several enzymes, including α-glucosidase, lipase, DPP-IV, and aldose reductase, along with limited effects on human cancer cell lines (IC50 > 10 μM). Despite its modest biological activity, Cyclocarin A may serve as a useful tool for research in enzyme inhibition and cancer biology. -
Cathepsin C Inhibitor
Verducatib is an orally active inhibitor of cathepsin C, also known as Dipeptidyl Peptidase I (DPP1). By inhibiting the activation of neutrophil serine proteases, Verducatib restores the balance of proteases and inhibitors, thereby reducing pulmonary inflammation and enhancing responses to infection. This compound has demonstrated efficacy in decreasing the frequency and severity of acute exacerbations in bronchiectasis, while also improving lung function and quality of life. Its safety profile is comparable to placebo, with a slight increase in mild-to-moderate cutaneous adverse events at higher doses, indicating potential for clinical application. -
DPP-4 Inhibitor
2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural compound that functions as a dipeptidyl peptidase-4 (DPP-4) inhibitor. It exhibits significant binding affinities to both DPP-4 and α-Amylase, suggesting its potential role in the regulation of glucose metabolism. This compound may offer beneficial effects in antidiabetic research, making it a valuable tool for studies focused on diabetes management and therapeutic development. -
Antidiabetic Compound
Lupinalbin A, a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor, demonstrates effective inhibition with IC50 values of 45.2 µM and 53.4 µM, respectively. This compound exhibits notable antidiabetic activity, making it a valuable tool for research in diabetes management and metabolic studies. Its dual inhibition profile supports investigations into glucose metabolism and insulin sensitivity. -
PDE1A1 Inhibitor
PDE1-IN-11 is a potent and selective inhibitor of phosphodiesterase 1A1 (PDE1A1). This compound enhances intracellular levels of cAMP and cGMP, thereby activating the PKA-CREB and NO-cGMP-PKG signaling pathways, which in turn promotes osteoblast differentiation and supports bone formation while inhibiting osteoclastogenesis and bone resorption. PDE1-IN-11 is a valuable tool for investigating postmenopausal osteoporosis and other disorders related to bone metabolism. -
Phosphodiesterase (PDE) Inhibitor
PDE10-IN-6 is a selective inhibitor of phosphodiesterase-10 (PDE10), which plays a crucial role in the degradation of cyclic AMP (cAMP) and cyclic GMP (cGMP). By inhibiting PDE10, this compound enhances the levels of these important second messengers, thereby affecting various signaling pathways. PDE10-IN-6 is primarily utilized in neurological research, specifically in studies related to cognitive function and neurodegenerative diseases. -
PDE-5 Inhibitor
BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor that elevates cGMP levels in tissues, enhancing the expression of nitric oxide (NO) and facilitating smooth muscle relaxation. This reagent is primarily utilized in research related to inflammation, immunology, and cardiovascular diseases, including conditions such as asthma and hypertension. Its ability to modulate cGMP signaling pathways makes it a valuable tool for investigating therapeutic strategies in these areas. -
PDE5 Inhibitor
UK 343664 is a selective inhibitor of phosphodiesterase 5 (PDE5), demonstrating significant potency and oral bioavailability. This compound has been shown to partially reverse thromboxane-induced pulmonary hypertension, indicating its potential therapeutic applications in treating cardiovascular disorders associated with pulmonary hypertension. -
PDE4 Inhibitor
CP-220629 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.44 μM. This compound is effective in mitigating airway obstruction, as evidenced by an ED50 of 2.0 mg/kg in guinea pig models using aerosolized antigen. CP-220629 is utilized in research aimed at exploring therapeutic strategies for respiratory conditions related to PDE4 activity. -
PDE10A Antagonist
AMG580 is a selective antagonist of phosphodiesterase 10A (PDE10A) with subnanomolar affinity across rat, primate, and human isoforms. This compound demonstrates significant biological activity in modulating intracellular signaling pathways associated with PDE10A inhibition. AMG580 is particularly useful in research applications involving noninvasive radiotracers, aiding in the exploration of brain imaging and neuropharmacology. -
PDE2 Agonist
5,6-DCl-cBIMP is a cyclic adenosine monophosphate (cAMP) analog that functions as an agonist of phosphodiesterase 2 (PDE2). This compound significantly enhances the hydrolytic activity of PDE2 on both cAMP and cGMP, making it a valuable tool for studying signal transduction pathways. Its potency and specificity position it as a useful reagent in research related to cardiovascular, neurological, and metabolic disorders. -
PDE4 Inhibitor
MK-0952 sodium is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, demonstrating an IC50 of 0.53 nM. This compound exhibits potential therapeutic effects in modulating inflammatory responses and cognitive functions, making it a valuable tool in Alzheimer’s disease research. MK-0952 sodium can be utilized to study the role of PDE4 in neurodegenerative disorders. -
PDE4 Inhibitor
UK-500001 is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating high potency with IC50 values of 0.28 nM for PDE4D3, 22.8 nM for PDE4B2, 26.1 nM for PDE4A4, and 271 nM for PDE4C2. This compound exhibits significant anti-inflammatory properties by effectively inhibiting the release of TNF-α and IFN-γ in both human and rodent macrophagic cell lines at nanomolar concentrations. UK-500001 holds potential for research applications in chronic obstructive pulmonary disease (COPD) and asthma treatment. -
PDE Inhibitor
Dazonone is a selective phosphodiesterase III (PDE3) inhibitor, exhibiting an IC50 of 1.68 μM. This compound enhances intracellular levels of cyclic AMP, leading to increased vasodilation and improved cardiac function. Dazonone is utilized in research on cardiovascular diseases and for investigating cellular signaling pathways involving cAMP modulation. -
PDE5 Inhibitor
N-Desethyl-N-methyl vardenafil is a potent PDE5 inhibitor, exhibiting an IC50 value of 0.14 μM. This compound is primarily utilized in pharmacological research focused on the modulation of erectile dysfunction and related cardiovascular conditions. Its capacity to inhibit PDE5 facilitates increased levels of cyclic GMP, thus enhancing vascular smooth muscle relaxation and blood flow. -
PDE Inhibitor
5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione is identified as a phosphodiesterase (PDE) inhibitor, specifically targeting both snake venom and human recombinant PDE 1 with IC50 values of 429 μM and 467 μM, respectively. Additionally, it exhibits weak inhibition of mushroom tyrosinase, with a calculated Ki of 1.9 μM. This compound can be utilized in biochemical research related to enzyme inhibition and potential pharmacological applications concerning PDE activity. -
PDE5 Inhibitor
Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 value of 3.95 ng/mL. This compound is primarily utilized in research related to erectile dysfunction, offering valuable insights into its mechanisms and potential therapeutic applications. -
Phosphodiesterase (PDE) Inhibitor
Hedgehog IN-8 is a potent phosphodiesterase (PDE) inhibitor that modulates hedgehog signaling pathways. This compound demonstrates significant biological activity in disrupting aberrant hedgehog signaling, which is often implicated in various cancers and developmental disorders. Hedgehog IN-8 is valuable for research applications aimed at understanding the role of hedgehog signaling in tumorigenesis and developing potential therapeutic interventions. -
PDE1/PDE5 Inhibitor
SCH 51866 is a potent and selective inhibitor of phosphodiesterase 1 (PDE1) and phosphodiesterase 5 (PDE5), with IC50 values of 70 nM and 60 nM, respectively. This compound effectively inhibits collagen-induced aggregation of human washed platelets with an IC50 of 10 μM and demonstrates protective effects against neointimal formation in balloon catheter-injured carotid arteries in spontaneously hypertensive rats. Additionally, SCH 51866 has been shown to reduce blood pressure in this model, making it a valuable tool for research in hypertension and related vascular disorders. -
TbrPDEB1 Inhibitor
Pyrazole N-Desmethyl sildenafil functions as an inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1). It demonstrates approximately 16% inhibition at a concentration of 100 µM. This compound is relevant for research into the pharmacological targeting of TbrPDEB1, which plays a role in the pathogenicity of Trypanosomiasis. -
PDE4 Inhibitor
AWD 12-281 is a potent and selective inhibitor of phosphodiesterase 4 (PDE4), with an IC50 of 9.7 nM. This compound demonstrates significant anti-inflammatory activity and is primarily utilized in research focused on allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis. Its oral bioavailability facilitates in vivo studies of PDE4 modulation in various inflammatory diseases. -
PDE Inhibitor
MP 518 is a phosphodiesterase (PDE) inhibitor that exhibits antihypertensive properties. By inhibiting the degradation of cyclic adenosine monophosphate (cAMP), MP 518 facilitates an increase in intracellular calcium (ICa) levels and antagonizes β-adrenergic stimulation, leading to vasodilation. This compound is valuable for research in cardiovascular biology and the mechanisms underlying hypertension. -
PDE Inhibitor
Pimobendan hydrochloride is a selective phosphodiesterase 3 (PDE3) inhibitor, with an IC50 value of 0.32 μM. It enhances cardiac contractility and promotes vasodilation, making it relevant for research into heart failure and other cardiovascular conditions. This compound can be utilized in studies exploring the modulation of cAMP levels and its effects on cardiac performance. -
Phosphodiesterase (PDE) Inhibitor
Dipyridamole Mono-O-β-D-glucuronide is an O-glucuronide derivative of Dipyridamole, a well-known phosphodiesterase (PDE) inhibitor. This compound exhibits significant inhibitory activity against PDE, which can influence cellular signaling pathways. Dipyridamole Mono-O-β-D-glucuronide is primarily utilized in research exploring drug metabolism and transport mechanisms, as well as in studies assessing the therapeutic potential of PDE inhibition.
