2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules.

Phosphodiesterase (PDE) Isoform Specific Products:

Phosphodiesterase (PDE) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W349178
    Medorinone
    		Inhibitor
    Medorinone is an inhibitor of cAMP phosphodiesterase activity. Medorinone can be used as a cardiac stimulant/vasodilator.
    Medorinone
  • HY-161936
    Z21115
    		Inhibitor
    Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg).
    Z21115
  • HY-122167
    L-869298
    		Inhibitor
    L-869298 is a potent and selective PDE4 inhibitor with an IC50 of 0.5 nM for PDE4A. L-869298 shows less active against hERG potassium channel.
    L-869298
  • HY-N2038R
    3,?5,?6,?7,?8,?3',?4'-?Heptemthoxyflavone (Standard)
    		Inhibitor
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone (Standard) is the analytical standard of 3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone (HY-N2038). This product is intended for research and analytical applications. 3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma.
    3,?5,?6,?7,?8,?3',?4'-?Heptemthoxyflavone (Standard)
  • HY-115511
    PyP-1
    		Inhibitor
    PyP-1 is a highly selective and potent PDE10 inhibitor. PyP-1 has a strong inhibitory effect on human PDE10A2 enzyme (Ki = 0.32 nM). PyP-1 can improve cognitive behavior. PyP-1 commonly used in research on conditions such as schizophrenia and cognitive impairment.
    PyP-1
  • HY-161290
    PDE5-IN-12
    		Inhibitor
    PDE5-IN-12 (compound 4h) is a potent phosphodiesterase-5 (PDE-5) inhibitor with an IC50 of 22 nM. PDE5-IN-12 shows anti-proliferative effects against the aortic cell line.
    PDE5-IN-12
  • HY-10679A
    PF-03049423
    		Inhibitor
    PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.
    PF-03049423
  • HY-B0442AS
    Vardenafil-d5 hydrochloride
    		Inhibitor 98.65%
    Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
    Vardenafil-d<sub>5</sub> hydrochloride
  • HY-170227
    Autotaxin-IN-7
    		Inhibitor
    Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis.
    Autotaxin-IN-7
  • HY-117181
    UK-1745
    		Inhibitor
    UK-1745 is a cardiotonic agent with vasodilating and antiarrhythmic properties. It increases intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes by inhibiting phosphodiesterase III, thereby enhancing myocardial contractility. Additionally, UK-1745 exhibits β-adrenergic receptor blocking activity, which helps reduce the oxygen consumption of the heart and prevent calcium overload. These characteristics make UK-1745 a promising candidate for research in congestive heart failure.
    UK-1745
  • HY-69172
    RS-25344
    		Inhibitor
    RS-25344 is a selective inhibitor of phosphodiesterase type IV (PDE4). RS-25344 increases intracellular cAMP (cyclic adenosine phosphate) concentration by inhibiting PDE4 activity. RS-25344 can be used in the study of inflammation, immune diseases, neurodegenerative diseases and cardiovascular diseases.
    RS-25344
  • HY-149661
    PDE5-IN-11
    		Inhibitor
    PDE5-IN-11 is a potent inhibitor of PDE5 with an IC50 of 40 nM. PDE5-IN-11 also inhibits PDE4 and PDE6 with IC50s of 1.78 and 0.09 μM, respectively.
    PDE5-IN-11
  • HY-175537
    ATX-IN-3
    		Inhibitor
    ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. ATX-IN-3 certainly reduces collagen deposition and ameliorates lung fibrosis in the pulmonary fibrosis mouse model. ATX-IN-3 has good metabolic stability and drug-like properties. ATX-IN-3 can used for the study of idiopathic pulmonary fibrosis (IFP).
    ATX-IN-3
  • HY-181774
    PDE4/5-IN-1
    		Inhibitor
    PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia.
    PDE4/5-IN-1
  • HY-182451
    V11294
    		Inhibitor
    V11294 is a phosphodiesterase 4 (PDE4) inhibitor with a Ki value of 436 nM against human lung PDE4. V11294 exhibits anti-inflammation activity.
    V11294
  • HY-147946
    PDE1-IN-4
    		Inhibitor
    PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.
    PDE1-IN-4
  • HY-124635
    BC-54
    		Inhibitor
    BC-54 is a selective inhibitor of enzymes from the cAMP-specific PDE4 and PDE7 families. BC-54 displays potent anti-inflammatory properties and can induce cancer cells apoptosis. BC-54 can be used for the researches of cancer and inflammation, such as chronic lymphocytic leukemia.
    BC-54
  • HY-12085S3
    Apremilast-d3
    		Inhibitor
    Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
    Apremilast-d<sub>3</sub>
  • HY-159654
    PDE4-IN-19
    		Inhibitor
    PDE4-IN-19 (compound 1) is a PDE4 inhibitor, with IC50 values of <10 nM and 10-100 nM for PDE4B1 and PDE4D3, respectively.
    PDE4-IN-19
  • HY-147950
    PDE4-IN-10
    		Inhibitor
    PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro.
    PDE4-IN-10
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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