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-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
  • HY-W074537
    P7-2104
    		Inhibitor 99.77%
    P7-2104 is a blood-brain barrier-permeable, selective PDE7A inhibitor with an IC50 of 31 nM. P7-2104 shows selectivity for hERG channels and most CYP450 subtypes. P7-2104 can be used for PDE7-targeted PET neuroimaging studies and research related to neurodegenerative diseases, when labeled with 11C or 18F.
    P7-2104
  • HY-169963
    PDE1-IN-8
    		Inhibitor
    PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model.
    PDE1-IN-8
  • HY-181981
    NTPDase/NPP1-IN-1
    		Inhibitor
    NTPDase/NPP1-IN-1 is an ectonucleotidase (NTPDase) and nucleotide pyrophosphatase/phosphodiesterase 1 (NPP1) inhibitor, with IC50 values of 0.28, 0.92, 0.82 and 0.73 μM against h-NTPDase1, h-NTPDase2, h-NTPDase3 and h-NPP1, respectively. NTPDase/NPP1-IN-1 is a membrane-interacting agent that localizes to the plasma membrane and interacts with cancer cells. NTPDase/NPP1-IN-1 can be used in the research of breast cancer.
    NTPDase/NPP1-IN-1
  • HY-119708A
    Ensifentrine tosylate
    		Inhibitor
    Ensifentrine (RPL-554) tosylate is an inhaled dual inhibitor of PDE3 and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine tosylate blocks PDE3 and PDE4 enzymes, thereby increasing the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, dilating the bronchi, and inhibiting the activation and migration of inflammatory cells. Ensifentrine tosylate can be used in the research of chronic obstructive pulmonary disease (COPD).
    Ensifentrine tosylate
  • HY-106804
    MS 857
    		Inhibitor
    MS 857 is an orally active nonglycoside and nonsympathomimetic cardiotonic agent. MS 857 exhibits cardiac and coronary vasodilator effect.
    MS 857
  • HY-114766
    Pumafentrine
    		Inhibitor
    Pumafentrine is an orally active, potent dual PDE3/PDE4 inhibitor. Pumafentrine dose-dependently ameliorates the clinical score and colonic TNFα production in murine Dextran sulphate sodium (DSS; HY-116282C)-induced colitis in a preventive setting.
    Pumafentrine
  • HY-W725737
    BrP-LPA
    		Inhibitor
    BrP-LPA is a LPA antagonist/ATX inhibitor. BrP-LPA shows pan-antagonist activity towards LPA1-4 GPCRs. BrP-LPA decreases blood vessel density. BrP-LPA dose-dependently inhibits Lysophosphatidic acid-induced head-dip counts. BrP-LPA exhibits anticancer activity against breast cancer, colon cancer, and lung cancer. BrP-LPA inhibits anxiety-like behavior.
    BrP-LPA
  • HY-100239
    ICI 153110
    		Inhibitor
    ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
    ICI 153110
  • HY-120195A
    PF-04827736
    		Inhibitor
    PF-04827736 (compound (S)-3) is a selective PDE1 inhibitor with IC50 values of 9.1 nM, 38 nM and 42 nM for PDE1B, PDE1C and PDE1A. PF-04827736 selectively inhibits human PDE1 over the other 10 superfamily members (PDE2-PDE11). PF-04827736 can be used for the study of cardiovascular disease.
    PF-04827736
  • HY-118938
    Hoquizil hydrochloride
    Hoquizil hydrochloride is a novel bronchodilator with oral activity, demonstrating phosphodiesterase inhibitory effects and potential for modulation of smooth muscle contraction.
    Hoquizil hydrochloride
  • HY-103084
    PDE5-IN-1
    		Inhibitor
    PDE5-IN-1 is an orally active, selective PDE5 inhibitor with an IC50 of 5.6 nM. PDE5-IN-1 forms hydrogen bond interactions with the Q817 residue in the catalytic domain of PDE5, and aromatic π-π stacking interactions with the F820 residue. PDE5-IN-1 exerts anti-cardiac hypertrophy and vasodilatory effects, reduces mean pulmonary arterial pressure and right ventricular hypertrophy index. PDE5-IN-1 can be used in the research of pulmonary arterial hypertension.
    PDE5-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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