Catalog No.
Product Name
Application
Product Information
Citations
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PDE-10A/A2AR Antagonist
PBF-999 is a dual antagonist of phosphodiesterase 10A (PDE-10A) and adenosine A2A receptors (A2AR). This compound exhibits significant modulation of intracellular signaling pathways, contributing to its potential in neuroscience research, particularly in studying disorders such as schizophrenia and Parkinson's disease. PBF-999 may facilitate insights into the therapeutic effects of PDE-10A and A2A receptor signaling in cognitive and motor function. -
PDE4 Inhibitor
Ronomilast is a potent phosphodiesterase-4 (PDE4) inhibitor, exhibiting an IC50 of 3 nM. This compound is primarily utilized in research focused on inflammation-related diseases. By inhibiting PDE4, Ronomilast increases intracellular cyclic AMP levels, thereby modulating inflammatory responses and offering insights into therapeutic strategies for various inflammatory conditions. -
CYP Isozymes Inhibitor
RPR203494 is a selective inhibitor of cytochrome P450 (CYP) isozymes, with significant activity against p38 mitogen-activated protein kinase, exhibiting an IC50 of 9 nM and an EC50 of 60 nM. This compound effectively inhibits hepatic CYP enzymes, making it a valuable tool in the study of drug metabolism and pharmacokinetics. RPR203494 holds potential for research applications related to rheumatoid arthritis and other inflammatory conditions, aiding in the exploration of therapeutic strategies targeting CYP-mediated pathways. -
NMT Inhibitor
MYX1715 is a potent inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. This compound effectively inhibits the proliferation of LU0884 and LU2511 cell lines, demonstrating IC50 values of 44 nM and 9 nM, respectively. MYX1715 has shown significant antitumor activity against neuroblastoma and gastric cancer in murine models, and it may be exploited as an antibody-drug conjugate (ADC) toxin for targeted cancer therapies. -
Nampt Inhibitor
Nampt-IN-10 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), exhibiting nanomolar inhibitory activity in various cancer cell lines, including MDA-MB453, NCI-N87, and NCI-H526. This compound can be utilized as a payload in antibody-drug conjugates (ADCs), where it has been shown to enhance anti-tumor efficacy. It serves as a valuable tool for researchers investigating NAMPT's role in cancer metabolism and therapeutic resistance. -
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. -
PDE11A Modulator
PDE11A modulator-1 is a selective modulator targeting phosphodiesterase 11A (PDE11A). This compound enhances intracellular cAMP levels, thereby influencing various signaling pathways. It has potential applications in the study of metabolic disorders and neurological conditions linked to cAMP signaling. PDE11A modulator-1 serves as a valuable tool for researchers investigating the role of PDE11A in cellular processes and therapeutic development. -
PDE IV Inhibitor
RS14203 is a potent inhibitor of phosphodiesterase type IV (PDE IV), which plays a crucial role in the regulation of cyclic nucleotide signaling. This compound is known to induce emesis, making it valuable in research focused on gastrointestinal function and the emetic response. Its application extends to investigations of PDE IV's involvement in various physiological processes and the development of therapeutic strategies targeting cyclic nucleotide pathways. -
PDE2 Inhibitor
BML-288 is a potent inhibitor of phosphodiesterase 2 (PDE2) with an IC50 value of 40 nM. This compound demonstrates significant biological activity in modulating cyclic nucleotide levels, making it relevant for research into osteoarthritis pain and related conditions. Its ability to selectively inhibit PDE2 provides valuable insights into cellular signaling pathways and therapeutic targets in inflammatory and pain-related disorders. -
Phosphodiesterase (PDE)
Oxagrelate is a selective inhibitor of cyclic adenosine monophosphate phosphodiesterase (PDE). It demonstrates concentration-dependent inhibition of platelet aggregation induced by collagen and adenosine diphosphate (ADP) in vitro. This compound is valuable for research applications focused on platelet activation, hemostasis, and thrombotic disorders. -
PDE5 Inhibitor
UK-371800 is a highly selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 of 4.2 nM. This compound demonstrates favorable permeability characteristics and remains unaffected by P-glycoprotein efflux mechanisms. UK-371800 is primarily utilized in research applications related to erectile dysfunction and pulmonary hypertension, contributing to the understanding of cGMP signaling pathways in cardiovascular health. -
PDE Inhibitor
PDE-IN-3 is a phosphodiesterase (PDE) inhibitor exhibiting an IC50 value of 260 μM. This compound effectively modulates the breakdown of cyclic nucleotides, making it a valuable tool for investigating intracellular signaling pathways. PDE-IN-3 is applicable in research areas such as cardiovascular biology, neurobiology, and cancer research, where PDE inhibitors play a critical role in therapeutic strategies. -
PDE5 Inhibitor
UK 357903 is a selective inhibitor of phosphodiesterase 5 (PDE5), exhibiting IC50 values of 1.7 nM for PDE5 and 714 nM for PDE6. This compound demonstrates significant vasodilatory effects in mesenteric and hindlimb vascular beds, making it a promising candidate for research applications related to erectile dysfunction and vascular smooth muscle relaxation. Its mechanism of action provides a valuable tool for investigating PDE5-related pathways in various physiological and pathological contexts. -
PDE4 Inhibitor
PDE4-IN-25 is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an IC50 value of 0.1 μM. This compound is significant in the study of inflammatory diseases, as it regulates intracellular cyclic nucleotide levels, thereby influencing inflammatory response pathways. PDE4-IN-25 is valuable for researchers investigating therapeutic interventions for conditions characterized by dysregulated inflammation. -
PDE4 Inhibitor
LEO 29102 is a potent inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 5 nM. This compound effectively inhibits the release of TNFα, making it a valuable tool for studies related to inflammatory responses. LEO 29102 shows promise in the research of atopic dermatitis and other related conditions associated with PDE4 activity. -
Cyclic AMP-PDE Inhibitor
2'-O-MB-cGMP sodium is a cyclic GMP-specific phosphodiesterase inhibitor with an I50 value of 35 µM. It effectively inhibits the hydrolysis of cyclic nucleotides by Ca2+-dependent phosphodiesterases, utilizing cAMP or cGMP as substrates. This compound is invaluable in research focused on cyclic nucleotide signaling pathways and can aid in the study of vascular smooth muscle function, platelet aggregation, and a range of physiological processes influenced by cyclic GMP. -
PDE5 Inhibitor
T-0156 free base is a selective inhibitor of phosphodiesterase type 5 (PDE5), functioning through competitive inhibition of cyclic guanosine monophosphate (cGMP) hydrolysis, with an IC50 of 0.23 nM. In addition to its primary target, T-0156 exhibits some inhibitory activity against PDE6 with an IC50 of 56 nM, while demonstrating low potency against other PDEs, including PDE1, PDE2, PDE3, and PDE4 (IC50 > 10 μM). This compound plays a valuable role in enhancing the nitric oxide (NO)/cGMP signaling pathway, making it suitable for research in vascular biology and therapies related to erectile dysfunction and pulmonary hypertension. -
PDE Inhibitor
Irsogladine maleate is a phosphodiesterase 4 (PDE4) inhibitor that enhances intracellular cyclic adenosine monophosphate (cAMP) levels. This compound exhibits anti-inflammatory properties and is primarily utilized in research focused on chronic inflammatory diseases and gastric protection mechanisms. Additionally, its affinity for muscarinic acetylcholine receptors may provide insights into neuroprotective effects and gastrointestinal motility studies. -
PDE III Inhibitor
Adibendan (BM 14478) is a selective phosphodiesterase III (PDE III) inhibitor, exhibiting an IC50 value of 2.0 μM. With over 60-fold selectivity compared to PDE I and II inhibitors, Adibendan functions as a novel cardiotonic agent. This compound is valuable for researchers investigating cardiovascular diseases and exploring the modulation of cardiac contractility through PDE III inhibition. -
PDE10A Inhibitor
Mardepodect precursor is the chemical precursor of Mardepodect, a selective inhibitor targeting phosphodiesterase 10A (PDE10A). This compound exhibits potent inhibitory activity with an IC50 of 0.37 nM and displays greater than 1000-fold selectivity over other phosphodiesterases. Mardepodect and its precursor are integral for research into neuropsychiatric disorders, promoting the understanding of PDE10A's role in central nervous system functions. -
PDE Inhibitor
LY 186126 is a potent phosphodiesterase (PDE) inhibitor that acts by targeting cardiac sarcoplasmic reticulum PDE with a high binding affinity (Kd = 5.6 nM). This compound is utilized in research related to cardiac function and signaling pathways by modulating cyclic nucleotide levels, making it valuable for studies on cardiovascular conditions and PDE-related mechanisms. -
PDE Inhibitor
Quazodine is a potent phosphodiesterase (PDE) inhibitor that modulates intracellular cAMP and cGMP levels. Its primary activity involves vasodilatory effects, making it a valuable tool in studies related to vascular smooth muscle function. Quazodine is suitable for research applications exploring cardiovascular diseases and smooth muscle physiology.
