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-126763
    ATI22-107
    		Inhibitor
    ATI22-107 is a dual-pharmacophore compound designed to simultaneously inhibit cardiac phosphodiesterase (PDE-III) and L-type calcium channels (LTCC), with activity that has specific effects on calcium cycling and contractility in cat ventricular myocytes and trabeculae.
    ATI22-107
  • HY-173483
    ATX inhibitor 26
    		Inhibitor
    ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model.
    ATX inhibitor 26
  • HY-90009B
    12-epi-Tadalafil
    		Inhibitor
    12-epi-Tadalafil is a PDE5 inhibitor (IC50: 0.09 μM). 12-epi-Tadalafil can be used for research of cardiovascular diseases.
    12-epi-Tadalafil
  • HY-120022
    THPP-2
    		Inhibitor
    THPP-2 is a tetrahydropyridopyrimidine-type phosphodiesterase 10A (PDE10A) inhibitor with a Ki of 94 nM. THPP-2 is applicable to the research of schizophrenia.
    THPP-2
  • HY-161506
    PDE1-IN-7
    		Inhibitor
    PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis.
    PDE1-IN-7
  • HY-177298
    PDE5-IN-15
    		Inhibitor
    PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC50 values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction.
    PDE5-IN-15
  • HY-157522
    NCI-14465
    		Inhibitor
    NCI-14465 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP1) inhibitor with an IC 50 of 26.4 μM. NCI-14465 can be used in cancer research.
    NCI-14465
  • HY-106088
    Tibenelast free acid
    		Inhibitor
    Tibenelast (LY186655) free acid is a potent and orally active is a phosphodiesterase inhibitor. Tibenelast free acid is an anti-asthma agent Tibenelast free acid increases the heart rate response to isoproterenol (HY-108353). Tibenelast free acid shows anti-anaphylactic shock activity. Tibenelast free acid has the potential for the research of asthma and other respiratory diseases.
    Tibenelast free acid
  • HY-132887
    PDE4-IN-3
    		Inhibitor
    PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).
    PDE4-IN-3
  • HY-161851
    MDL3
    		Inhibitor
    MDL3 is a novel inhibitor of PDE4B and PDE5A. MDL3 against liver injury and inflammation and inhibits the pathological remodeling of adipose tissue.
    MDL3
  • HY-14252S
    Milrinone-d3
    		Inhibitor
    Milrinone-d3 is deuterium labeled Milrinone. Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
    Milrinone-d<sub>3</sub>
  • HY-16900G
    Rolipram (GMP)
    		Inhibitor
    Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.
    Rolipram (GMP)
  • HY-162911
    Enpp-1-IN-22
    		Inhibitor
    Enpp-1-IN-22 is an orally bioavailable prodrug of the potent ENPP1 inhibitor paraformaldehyde with antitumor activity.
    Enpp-1-IN-22
  • HY-108620
    CDP-840
    		Inhibitor
    CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys.
    CDP-840
  • HY-106245
    HT-0712
    		Inhibitor
    HT-0712 is a Phosphodiesterase Type 4 (PDE4) inhibitor. HT-0712 enhances rehabilitation-dependent motor recovery and cortical reorganization after focal cortical ischemia.
    HT-0712
  • HY-135089
    Autotaxin-IN-5
    		Inhibitor
    Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis.
    Autotaxin-IN-5
  • HY-126754
    Archangelicin
    		Inhibitor
    Archangelicin is an inhibitor for cAMP-phosphodiesterase (cAMP-PDE) with IC50 >400 μM. Archangelicin inhibits nuclear factor of activated T cell (NFAT) with IC50 of 9 μM. Archangelicin exhibits antitumor and anti-inflammatory.
    Archangelicin
  • HY-N17617
    S-Petasin
    		Inhibitor
    S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis.
    S-Petasin
  • HY-172776
    Phosphodiesterase-IN-3
    		Inhibitor
    Phosphodiesterase-IN-3 (Example 20) is a phosphodiesterase 4B inhibitor, with IC50s of <10 nM and 10-100 nM for PDE4B1 and PDE4D3, respectively. Phosphodiesterase-IN-3 has the potential for the research of idiopathic pulmonary fibrosis.
    Phosphodiesterase-IN-3
  • HY-113822
    Lixazinone hydrogensulfate
    		Inhibitor
    Lixazinone (RS-82856) hydrogensulfate is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone hydrogensulfate exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone hydrogensulfate increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [32P]cGMP. Lixazinone hydrogensulfate can be used in the research of polycystic kidney disease and congestive heart failure.
    Lixazinone hydrogensulfate
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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