Catalog No.
Product Name
Application
Product Information
Citations
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Phosphodiesterase (PDE) Inhibitor
K-252d is an indolocarbazole alkaloid that acts primarily as a phosphodiesterase (PDE) inhibitor. It demonstrates significant inhibitory activity against calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart, with an IC50 of 46.2 μM, and is also recognized for its role as a protein kinase C (PKC) inhibitor, exhibiting an IC50 of 350 nM against PKC isolated from rat brain. This compound is valuable for studies related to signal transduction pathways and therapeutic interventions targeting PDE-related disorders. -
PDE Stabilizer
6-Cl-cPuMP sodium is a cAMP analog that acts as a phosphodiesterase (PDE) stabilizer. This compound exhibits excellent membrane permeability, allowing for effective cellular uptake, while maintaining stability against PDE degradation. 6-Cl-cPuMP sodium is particularly useful in research related to the nervous system, enabling studies of cAMP signaling pathways and their implications in neurobiology. -
PDE4 Inhibitor
Cipamfylline is a potent inhibitor of phosphodiesterase 4 (PDE4), specifically facilitating the accumulation of PDE4A4 within distinct cellular regions via its interaction with the ubiquitin scaffolding protein p62. This compound plays a critical role in research focused on atopic dermatitis, contributing to the understanding of inflammatory pathways and potential therapeutic interventions in this condition. -
PDE4 Inhibitor
ONO-6126 is a selective phosphodiesterase 4 (PDE4) inhibitor with potential therapeutic applications in respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). By inhibiting PDE4, it increases intracellular cAMP levels, which can help reduce inflammation and bronchoconstriction. This compound is valuable for research focused on understanding the molecular mechanisms of respiratory conditions and testing novel therapeutic strategies. -
PDE4 Inhibitor
Braylin is a potent phosphodiesterase-4 (PDE4) inhibitor that plays a significant role in anti-inflammatory and immunomodulatory processes. It is particularly relevant in the exploration of immunoinflammatory diseases, making it a valuable tool for researchers studying these conditions. Its ability to modulate inflammatory responses positions it as a potential therapeutic target in related research applications. -
PDE4 Inhibitor
RS-25344 is a selective inhibitor of phosphodiesterase type IV (PDE4), which plays a crucial role in the degradation of cyclic adenosine monophosphate (cAMP). By inhibiting PDE4 activity, RS-25344 promotes increased intracellular cAMP levels, contributing to an array of biological responses. This compound is valuable for research in inflammation, immune disorders, neurodegenerative diseases, and cardiovascular conditions. Its ability to modulate cAMP signaling makes it a significant tool for exploring therapeutic strategies in these areas. -
PDE5 Inhibitor
Desmethyl thiosildenafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. This compound exhibits significant biological activity by promoting vasodilation through the inhibition of PDE5, thereby enhancing nitric oxide signaling. It is commonly used in research applications focused on cardiovascular function and erectile dysfunction, providing insights into the therapeutic potential for related disorders. -
PDE5 Inhibitor
JNJ-10258859 is a highly selective phosphodiesterase type 5 (PDE5) inhibitor, exhibiting a Ki value of 0.23 nM. This compound effectively elevates cyclic GMP levels, which is crucial for promoting smooth muscle relaxation and improving erectile function. JNJ-10258859 is primarily utilized in research focused on erectile dysfunction and related cardiovascular studies. -
PDE2 Agonist
5,6-DM-cBIMP is a cyclic nucleotide analog that serves as an agonist for phosphodiesterase 2 (PDE2). It is capable of significantly enhancing the hydrolytic activities of cAMP and cGMP by PDE2, making it a valuable tool for researchers investigating the modulation of cyclic nucleotide signaling pathways. Its application is particularly relevant in studies focused on cardiovascular and neurological research. -
PDE1 Inhibitor
MMPX is a potent phosphodiesterase type 1 (PDE1) inhibitor that modulates intracellular signaling pathways by increasing cyclic nucleotide levels. This compound exhibits significant biological activity in various cellular processes, making it a valuable tool for studying the physiological roles of PDE1 in neurological and cardiovascular research. Its application extends to exploring therapeutic strategies for diseases associated with dysregulated cyclic nucleotide signaling. -
PDE5 Inhibitor
BMS-341400 mesylate is a selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 value of 0.3 nM. This compound attenuates the degradation of cyclic guanosine monophosphate (cGMP), thereby facilitating nitric oxide (NO)-induced relaxation of corpus cavernosum smooth muscle and enhancing erectile function. BMS-341400 mesylate serves as a valuable tool for investigating mechanisms underlying erectile dysfunction. -
KRAS-PDEδ Inhibitor
NHTD is a selective inhibitor of KRAS-PDEδ, targeting the prenyl-binding pocket of PDEδ and modulating the cellular localization of KRAS. This action effectively inhibits the proliferation of KRAS-mutant cancer cells and promotes apoptosis. NHTD is a valuable tool for investigations into KRAS-driven non-small cell lung cancer (NSCLC) and related oncology research. -
Phosphodiesterase (PDE) Inhibitor
Saterinone is a phosphodiesterase III (PDE III) inhibitor that enhances intracellular cAMP levels, leading to increased vasodilation and improved cardiac function. This compound is significant in cardiovascular research, particularly in studies focused on heart failure and angina. Its role in modulating cAMP signaling pathways makes it an important tool for exploring therapeutic strategies in cardiovascular diseases. -
Phosphodiesterase (PDE) Inhibitor
PDE IV-IN-1 is a selective inhibitor of phosphodiesterase IV (PDE4), an enzyme involved in the degradation of cyclic AMP. This compound exhibits anti-inflammatory properties, making it valuable for the research of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD), as well as other inflammatory diseases. Its ability to modulate cAMP levels positions PDE IV-IN-1 as a significant tool in the study of inflammatory signaling pathways. -
Phosphodiesterase (PDE) Inhibitor
L791943 is a selective phosphodiesterase-4 (PDE4) inhibitor, demonstrating a potent inhibitory effect with an IC50 value of 4.2 nM. This compound is primarily utilized in research aimed at understanding the role of PDE4 in various inflammatory and neurological disorders. Its efficacy in modulating cyclic nucleotide levels makes it a valuable tool for studying signal transduction pathways and therapeutic interventions. -
Phosphodiesterase (PDE) Inhibitor
Sch59498 is a potent inhibitor of phosphodiesterase 1C (PDE1C), a phosphodiesterase enzyme involved in cellular signal transduction through the hydrolysis of cyclic nucleotides. This compound demonstrates significant effects on intracellular cAMP and cGMP levels, thereby influencing various physiological processes. Sch59498 is primarily utilized in research applications focused on cardiovascular diseases, neuroprotection, and cancer biology, providing insights into the modulation of signaling pathways associated with these conditions. -
Phosphodiesterase (PDE) Inhibitor
Win-62005 is a potent inhibitor of cyclic AMP phosphodiesterase III (PDE III), exhibiting Ki values of 25 nM for rat heart and 26 nM for canine aorta. This compound is primarily utilized in cardiovascular research to explore its effects on cAMP signaling pathways and its potential therapeutic applications in heart conditions. Through the inhibition of PDE III, Win-62005 enhances intracellular cAMP levels, thereby influencing myocardial contractility and vascular tone. -
Cathepsin A Substrate
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative that serves as a specific substrate for Cathepsin A. This compound is valuable in elucidating the enzymatic activity and functional mechanisms of Cathepsin A, contributing to research on its role in physiological and pathological processes. FA-Phe-Phe is particularly useful in studies involving enzymatic assays and screening for potential inhibitors or modulators of Cathepsin A. -
PKCα Inhibitor
Leucosceptoside A is a phenylethanoid glycoside that functions as a selective inhibitor of Protein Kinase C alpha (PKCα). This compound demonstrates significant anti-hyperglycemic and anti-hypertensive effects and exhibits inhibitory activity against α-glucosidase, with an IC50 value of 19.0 μM. Leucosceptoside A is relevant for research into metabolic disorders and cardiovascular diseases, providing insights into therapeutic approaches targeting PKCα. -
Fluorochrome
DDAO phosphate diammonium is a fluorescent phosphatase substrate that serves as a sensitive probe for enzyme activity. With tunable excitation wavelengths ranging from 600 to 650 nm and a long emission wavelength of 656 nm, it facilitates the detection of various enzymes including β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin, and esterase. This reagent is ideal for applications in enzymology and biochemistry research, enabling real-time monitoring of enzyme activities in different biological systems. -
TrxR Fuorescence Probe
Seph-PAO is a modified para-aminooxyphenyl (PAO) compound conjugated with a sepharose fluorophore, designed to selectively detect thioredoxin reductase (TrxR). This fluorescence probe demonstrates high sensitivity and specificity, facilitating the study of TrxR activity in various biological systems. Researchers can employ Seph-PAO in investigations of oxidative stress, redox signaling, and the role of TrxR in cellular processes. -
Carboxylesterase Substrate, Mitochondria Targeting Agent
CEMT is a selective substrate for carboxylesterases, functioning as a ratiometric two-photon fluorescent reporter probe. Upon hydrolysis by carboxylesterases, CEMT generates HMT, which facilitates mitochondrial pH sensing through ratiometric fluorescence changes in response to pH fluctuations. This compound specifically targets and covalently binds to mitochondria, minimizing leakage during acidification, thereby enabling in situ imaging of mitochondrial dynamics and pH variations within biological systems. -
CYP1B1
CYP1B1-IN-6 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1. This compound demonstrates the ability to inhibit CYP1B1 activity, making it useful for tumor identification in fluorescence and photoacoustic imaging modalities. CYP1B1-IN-6 can assist in research applications focused on cancer diagnostics and the investigation of metabolic processes involving CYP1B1. -
ALOX12-ACC1 interaction inhibitor
IMA-1 is an inhibitor of the interaction between arachidonic acid 12-lipoxygenase (ALOX12) and acetyl-CoA carboxylase 1 (ACC1). This compound has demonstrated significant efficacy in blocking the progression of diet-induced non-alcoholic steatohepatitis (NASH) in male mice and crab-eating monkeys, while not inducing hyperlipidemia. IMA-1 serves as a valuable tool for investigating the underlying mechanisms and potential treatments for NASH. -
Herbicide
Sethoxydim is a postemergent herbicide that specifically targets acetyl-coenzyme A carboxylase (ACCase) activity in plants. By inhibiting this key enzyme, Sethoxydim effectively disrupts fatty acid biosynthesis, leading to the control of various grass weeds in a range of crop systems. This compound is widely utilized in agricultural research to study herbicide resistance mechanisms and weed management strategies. -
Herbicide
Haloxyfop is an aryloxyphenoxypropionic acid herbicide that primarily targets acetyl coenzyme A carboxylase (EC 6.4.1.2) in corn seedling chloroplasts, exhibiting an IC50 value of 0.5 μM. This compound effectively controls grass weeds in broad-leaf crops, making it a valuable tool in agricultural research. Its selective action enhances studies on herbicide resistance and crop management strategies. -
Herbicide
Quizalofop is a selective herbicide that targets acetyl-CoA carboxylase (ACCase), leading to the inhibition of fatty acid synthesis in plants. This compound is instrumental in agricultural research and can be utilized to screen EMS mutated microalgae, facilitating investigations aimed at enhancing microalgae biofuel production efficiency.
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Herbicide
Quizalofop-P is a selective herbicide that targets the inhibition of cellular fatty acid synthesis in plants. It is effectively absorbed through the leaves and stems of weed species, leading to upward and downward translocation and accumulation in meristematic regions. This compound induces necrosis in grass weeds while exhibiting minimal impact on dicotyledonous crops, making it a valuable tool in agricultural applications for effective weed management. -
Herbicide
Fluazifop is a selective herbicide that functions by inhibiting acetyl-CoA carboxylase, an enzyme critical for fatty acid synthesis in plants. This inhibition disrupts the growth of specific grass species while sparing broadleaf plants, making it valuable in agricultural applications for weed management. Fluazifop is particularly effective in controlling post-emergent grass weeds, contributing to improved crop yields and sustainable farming practices. -
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.
