Catalog No.
Product Name
Application
Product Information
Citations
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picomolar PDE1 inhibitor
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). -
PDEδ inhibitor
Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM. -
PDEδ inhibitor
Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM. -
Autotaxin Inhibitor IV
HA155, also known as Autotaxin Inhibitor IV, is a boronic acid-based compound that inhibits autotaxin (IC50 = 5.7 nM) by selectively binding to its catalytic threonine. - Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
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enpp-1 inhibitor
Enpp-1-IN-1 is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor extracted from patent WO2019046778, Example 55. -
PDE4 inhibitor
Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM. -
PDE4/NF-κB inhibitor
Sappanone A is an orally active homoisoflavone isolated from Caesalpinia sappan L., exhibiting notable anti-inflammatory and antioxidant properties. It functions as an inhibitor of phosphodiesterase 4 (PDE4) and NF-κB, key regulators of inflammatory signaling. Additionally, Sappanone A activates the Nrf2 pathway, leading to increased expression of the cytoprotective enzyme heme oxygenase-1 (HO-1). Sappanone A also inhibits RANKL-induced osteoclastogenesis, suggesting potential benefits in bone metabolism disorders. With its multifaceted bioactivity, Sappanone A holds significant promise for research in inflammation-related diseases, cardiovascular conditions, and bone health. -
PDE6D/IKZF1/IKZF3/CK1α Degrader
FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
PDE Inhibitor
Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD). -
PDE4 Inhibitor
PDE4-IN-10 is a selective phosphodiesterase 4 (PDE4) inhibitor, exhibiting an IC50 of 7.01 μM for the PDE4B isoform. This compound demonstrates significant biological activity by inhibiting TNF-α production and exhibits microsomal stability, making it suitable for various in vitro applications. PDE4-IN-10 is a valuable tool for research aimed at understanding inflammatory processes and developing therapeutic strategies for related diseases. -
PDE Inhibitor
Theophylline L-lysine is a soluble derivative of Theophylline that primarily acts as a phosphodiesterase (PDE) inhibitor. It effectively inhibits PDE3 activity, which leads to relaxation of airway smooth muscle and exhibits anti-inflammatory properties through the enhancement of IL-10 levels and the inhibition of NF-κB nuclear translocation. Additionally, Theophylline L-lysine induces apoptosis, making it a valuable compound for research applications in asthma and chronic obstructive pulmonary disease (COPD). -
PDE4 PROTAC Degrader
PROTAC PDE4 degrader-1 is a selective and orally active degrader targeting phosphodiesterase 4 (PDE4). It exhibits a DC50 of 41.98 μM and effectively inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. This compound demonstrates significant potential in alleviating pulmonary inflammation in LPS-induced acute lung injury models, making it a valuable tool for studying inflammatory diseases and therapeutic interventions. -
PDE4 Inhibitor
AN-2898 is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 0.027 μM, demonstrating significant potency over other phosphodiesterase enzymes, including PDE1A, PDE2A, and PDE3A. It effectively inhibits PDE4 subtypes such as PDE4B1, PDE4A1A, and PDE4D2. AN-2898 significantly reduces the production of pro-inflammatory cytokines including TNF-α, IL-2, IFN-γ, IL-5, and IL-10, making it a valuable reagent for research applications in mild to moderate atopic dermatitis and psoriasis. -
PDE4 Inhibitor
LY2775240 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating significant inhibitory activity against PDE4A, PDE4B, and PDE4D with IC₅₀ values of 0.09 nM and 0.14 nM for the latter two, as well as an IC₅₀ of 2.4 nM for PDE4C. This compound effectively reduces TNFα production during immune activation, making it valuable for studies investigating inflammatory conditions. LY2775240 is particularly relevant for research focused on psoriasis, as evidenced by its efficacy in lowering TNFα levels in rodent and cynomolgus monkey models. -
PDE4 Inhibitor
ASP9831 is an orally active phosphodiesterase type 4 (PDE4) inhibitor. It effectively inhibits lipopolysaccharide (LPS)-induced tumor necrosis factor-alpha (TNF-α) production, demonstrating notable anti-inflammatory properties. This compound is valuable for research applications centered on fatty liver disease and related inflammatory conditions. -
PDE4 Inhibitor
Revamilast is an orally active phosphodiesterase-4 (PDE4) inhibitor with a reported IC50 of 3 nM. This compound effectively inhibits the production of tumor necrosis factor-alpha (TNF-α), making it a valuable tool for research into inflammatory conditions. Applications include studies related to rheumatoid arthritis, plaque psoriasis, asthma, and other related inflammatory diseases. -
PDE4 Inhibitor
PDE4-IN-15 is a selective inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 0.17 μM. This compound demonstrates notable anti-TNF-α activity, exhibiting an EC50 of 0.19 μM, which is significant for inflammatory research. Additionally, PDE4-IN-15 shows good skin permeability, making it suitable for studies involving topical administration and localized therapeutic applications. -
PDE Inhibitor
Theophylline sodium glycinate is a potent phosphodiesterase (PDE) inhibitor with significant effects on airway smooth muscle relaxation. It acts primarily by inhibiting PDE3, which contributes to its anti-inflammatory properties through the upregulation of IL-10 and the inhibition of NF-κB translocation into the nucleus. Additionally, Theophylline sodium glycinate has been shown to induce apoptosis. This reagent is valuable for research applications related to asthma and chronic obstructive pulmonary disease (COPD). -
PDE-4 Inhibitor
Apremilast-d5 is a deuterated analog of Apremilast, a potent inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. This compound effectively reduces TNF-α release in response to lipopolysaccharide (LPS) stimulation, exhibiting an IC50 of 104 nM. Apremilast-d5 is valuable for research applications related to inflammatory diseases and the modulation of immune responses. -
Phosphodiesterase (PDE) Inhibitor
CDC801 is a potent inhibitor of phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α), with IC50 values of 1.1 μM and 2.5 μM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into conditions associated with elevated TNF-α levels, such as autoimmune diseases and chronic inflammatory disorders. CDC801 is suitable for exploring the therapeutic potential of PDE4 inhibition and its effects on inflammatory pathways. -
PDE Inhibitor
Theophylline monohydrate is a potent phosphodiesterase (PDE) inhibitor that primarily targets PDE3, promoting relaxation of airway smooth muscle. This compound exhibits anti-inflammatory properties by increasing interleukin-10 (IL-10) levels and inhibiting the nuclear translocation of NF-κB. Additionally, Theophylline monohydrate is known to induce apoptosis in certain cell types. It is widely utilized in research related to asthma and chronic obstructive pulmonary disease (COPD). -
HDAC/PDE5 Inhibitor
CM-414 is a potent dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDACs), exhibiting IC50 values of 60 nM for PDE5 and ranging from 91 nM to 490 nM for various HDAC isoforms, including HDAC6 and HDAC1. This compound effectively reduces levels of amyloid-beta (Aβ) and phosphorylated tau (pTau) in Tg2576 mouse models, making it a valuable tool for Alzheimer's disease research. Its ability to penetrate the blood-brain barrier enhances its potential for studying neurodegenerative disorders and therapeutic interventions. -
HDAC/PDE5 Inhibitor
CM-545 is a dual inhibitor targeting both histone deacetylases (HDACs) and phosphodiesterase 5 (PDE5). With pIC50 values of 7.47 for PDE5, 6.65 for HDAC1, 6.14 for HDAC2, 6.55 for HDAC3, and 6.84 for HDAC6, CM-545 demonstrates potent inhibitory activity. This compound has applications in cancer research and therapeutic interventions related to neurodegenerative diseases and cardiovascular conditions, owing to its modulation of histone acetylation and cyclic nucleotide signaling pathways. -
PDEIII Inhibitor
Anagrelide hydrochloride is a selective phosphodiesterase type III (PDE3) inhibitor with an IC50 value of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and suppresses megakaryocyte development in the bone marrow. Additionally, Anagrelide hydrochloride has been shown to reduce the proliferation of gastrointestinal stromal tumor (GIST) cells and induce apoptosis in vitro, highlighting its potential as an antineoplastic agent. Its primary application lies in its role as a platelet-lowering agent with antithrombopoietic properties. -
PDE IV Inhibitor/A1AR Antagonist
Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm. -
PDE Inhibitor
Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches. -
PDE5 Inhibitor
Vardenafil hydrochloride trihydrate is a selective and orally active phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. It also demonstrates inhibitory effects on PDE1 and PDE6 with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4 (IC50s >1000 nM). By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride trihydrate elevates cGMP levels. This compound is primarily utilized in research related to erectile dysfunction as well as conditions such as hepatitis and diabetes. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
PDE Inhibitor
Pentoxifylline is a non-selective phosphodiesterase (PDE) inhibitor with significant haemorheological properties. It exhibits immune modulation, anti-inflammatory, anti-fibrinolytic, and anti-proliferative activities, making it a valuable tool in biomedical research. Pentoxifylline is particularly applicable in studies of peripheral vascular disease, cerebrovascular disease, and other conditions associated with impaired regional microcirculation. -
PDE5 Inhibitor
Vardenafil hydrochloride is a selective phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. This compound demonstrates moderate inhibition of PDE1 and PDE6, with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4. By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride effectively elevates cGMP levels. It serves as a valuable tool in research related to erectile dysfunction, hepatitis, and diabetes. -
PDE3A Modulator
Nauclefine is an indole alkaloid derived from Nauclea officinalis, serving as a modulator of phosphodiesterase 3A (PDE3A). This compound has been shown to promote apoptosis in cancer cells via a PDE3A-SLFN12-dependent death pathway. Its biological activity makes Nauclefine a valuable tool for research into cancer therapeutics and the understanding of apoptotic mechanisms. -
PDE1 Inhibitor
PDE1-IN-6 is a selective phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 7.5 nM. It effectively inhibits cell proliferation and induces apoptosis in acute myelogenous leukemia (AML) cells. This compound serves as a valuable tool in cancer research, particularly in studies focused on signaling pathways involved in leukemia progression and treatment. -
PDE6/NAMPT Inhibitor
PDEδ/NAMPT IN-1 is a potent dual inhibitor targeting phosphodiesterase 6 (PDE6) with a binding affinity of 0.410 nM and nicotinamide phosphoribosyl transferase (NAMPT) with an IC50 of 2.21 nM. This compound effectively disrupts KRAS-related signaling pathways and hampers the synthesis of nicotinamide adenine dinucleotide (NAD+), leading to apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 holds significant potential for advancing research in KRAS mutant pancreatic cancer. -
Calcium Sensitiser
OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies. -
PDEIII Inhibitor
Anagrelide is a potent phosphodiesterase type III (PDE3) inhibitor with an IC50 of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and attenuates megakaryocytopoiesis in the bone marrow. Additionally, Anagrelide demonstrates the capacity to reduce proliferation and promote apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro. Its primary application includes functioning as a platelet-lowering agent with significant antithrombopoietic properties. -
PDE4/7 Inhibitor
BC-54 is a selective inhibitor of phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7). It exhibits potent anti-inflammatory effects and can induce apoptosis in cancer cells, making it a valuable tool for research focused on cancer and inflammation. BC-54 is particularly relevant in studies investigating chronic lymphocytic leukemia and other conditions associated with these pathways. -
PDE4 Inhibitor
CC-3052 is a selective phosphodiesterase 4 (PDE4) inhibitor exhibiting immunomodulatory properties. It effectively reduces neutrophil apoptosis in HIV-positive contexts, highlighting its potential in the study of HIV-related diseases. This compound serves as a valuable tool for researchers investigating the modulation of immune responses in viral infections. -
PDE5 Inhibitor
PDE5-IN-3 is a potent phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 of 1.57 nM. In addition to its primary mechanism, PDE5-IN-3 demonstrates moderate inhibition of epidermal growth factor receptor (EGFR) with an IC50 of 5.827 µM and significantly affects the Wnt/β-catenin signaling pathway with an IC50 of 1286.96 ng/mL. This compound has been shown to induce the intrinsic apoptotic mitochondrial pathway in HepG2 cells and displays strong antitumor activity, making it valuable for cancer research applications. -
PDE5/HDAC Inhibitor
PDE5/HDAC-IN-1 is a dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) with IC50 values of 46.3 nM and 14.5 nM, respectively. This compound has demonstrated the capability to induce cell apoptosis and exhibits significant anticancer activities. PDE5/HDAC-IN-1 is a valuable tool for research in cancer therapeutics and epigenetic modulation. -
PDEIII Inhibitor
Anagrelide hydrochloride monohydrate is a selective inhibitor of phosphodiesterase type III (PDE3), with an IC50 value of 36 nM. This imidazoquinazoline derivative effectively inhibits platelet aggregation and reduces bone marrow megakaryocytopoiesis. Additionally, Anagrelide hydrochloride monohydrate demonstrates the capability to decrease cell proliferation and induce apoptosis in gastrointestinal stromal tumor (GIST) cells in vitro, making it relevant for research in hematology and oncology. Its platelet-lowering properties contribute to its antithrombopoietic effects. -
PDE4 Inhibitor
GPD-1116 is a potent inhibitor of Phosphodiesterase (PDE) 4 and PDE1, demonstrating oral bioactivity. This compound effectively reduces smoke-induced apoptosis in lung cells, making it relevant for respiratory research. GPD-1116 shows promise in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary hypertension, supporting its potential therapeutic applications in pulmonary disorders. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
PDE4 Inhibitor
Morcamilast is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, exhibiting IC50 values of 1.28 nM for PDE4A1A, 2.33 nM for PDE4B1, and 1.63 nM for PDE4D2. This compound demonstrates significant anti-inflammatory activity by inhibiting the lipopolysaccharide (LPS)-induced release of pro-inflammatory cytokines, including TNF-α, IL-12/23p40, IL-23, and IL-17A in human peripheral blood mononuclear cells (PBMCs) and T cells. Morcamilast also exhibits antipruritic effects, making it a valuable tool for investigating psoriasis, atopic dermatitis, and various other inflammatory disorders. -
PDE1C Inhibitor
PDE1-IN-9 is a selective inhibitor of phosphodiesterase 1 (PDE1), demonstrating an IC50 of 11 nM for PDE1C. This compound significantly reduces the mRNA expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α, as well as iNOS, while inhibiting the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 also showcases favorable metabolic stability in rat liver microsomes, making it a valuable tool for studying PDE1-related pathways and inflammatory responses. -
PDE4 Inhibitor
Mesopram is a selective phosphodiesterase (PDE) 4 inhibitor that effectively reduces the synthesis of pro-inflammatory cytokines, including TNF-α and IFN-γ. This compound has shown efficacy in alleviating Dextran sulfate sodium (DSS)-induced colitis in murine models, making it a valuable tool for research in chronic inflammatory diseases. Mesopram can be employed to investigate therapeutic strategies aimed at modulating inflammatory responses.
