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-153398
    Enpp-1-IN-17
    		Inhibitor
    Enpp-1-IN-17 (example 274) is a potent ENPP1 inhibitor, with the inhibition constants (Ki values) toward cGAMP and ATP hydrolysis of 100 nM-1 μM and > 1 μM, respectively. The selectivity ratio for inhibition of cGAMP hydrolysis versus ATP hydrolysis is >6.4.
    Enpp-1-IN-17
  • HY-128060
    PDE5-IN-42
    		Inhibitor
    PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC50 of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11.
    PDE5-IN-42
  • HY-144684
    PDE4-IN-8
    		Inhibitor
    PDE4-IN-8 (Example 5) is a potent PDE4 inhibitor with an IC50 of 0.93 nM for PDE4B2.PDE4-IN-8 has little effect on IL13 (IC50=4.04 nM), IL4 (IC50=36.33 nM), IFNy (IC50=2394 nM).
    PDE4-IN-8
  • HY-18252S
    Avanafil-13C,d3
    		Inhibitor
    Avanafil-13C,d3 is the 13C- and deuterium labeled Avanafil.
    Avanafil-<sup>13</sup>C,d<sub>3</sub>
  • HY-134954
    Palmitoleoyl 3-carbacyclic phosphatidic acid
    		Inhibitor
    Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) is an intermediately potent inhibitor of autotaxin (ATX) with an IC50 of 620 nM. Palmitoleoyl 3-carbacyclic phosphatidic acid can be used for melanoma research.
    Palmitoleoyl 3-carbacyclic phosphatidic acid
  • HY-108622
    Mesopram
    		Inhibitor 98.80%
    Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. Mesopram can be used for autoimmune disease research.
    Mesopram
  • HY-126167
    Deacetylsclerotiorin
    		Inhibitor
    Deacetylsclerotiorin is a secondary metabolite of chloramphenicol isolated from the fungus Bartalinia robillardoides strain LF550. Deacetylsclerotiorin has significant inhibitory effects on Candida albicans (IC50=24 μM), Trichophyton rubrum (IC50=2.83 μM) and Septoria tritici (IC50=7..45 μM). In addition, Deacetylsclerotiorin also exhibits inhibitory effects on the enzyme phosphodiesterase 4 (PDE4) (IC50=2.8 μM).
    Deacetylsclerotiorin
  • HY-143582
    ATX inhibitor 9
    		Inhibitor
    ATX inhibitor 9 is a potent inhibitor of ATX. ATX inhibitor 9 is a thickened heteroaryl derivatives compound. Autotaxin (ATX), also known as ENPP2, is a secreted enzyme that is highly expressed mainly in cancer cells, bronchial epithelial cells and alveolar macrophages in the lung. ATX inhibitor 9 has the potential for the research of cancer or fibrous degenerative disease (extracted from patent WO2021078227A1, compound 3).
    ATX inhibitor 9
  • HY-153168
    Bemoradan
    		Inhibitor
    Bemoradan (compound 10a) is an orally active and selective canine Phosphodiesterase (PDE) fraction III inhibitor. Bemoradan is a long-acting, potent, inotropic vasodilator and a novel cardiotonic agent, and can be used in congestive heart failure research.
    Bemoradan
  • HY-B0809B
    Theophylline sodium acetate
    		Inhibitor
    Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline sodium acetate
  • HY-160111
    PDM-042
    		Inhibitor
    PDM-042 is a potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor. PDM-042 shows potent inhibitory activities for human and rat PDE10A with IC50 values of less than 1 nM and more than 1000-fold selectivity against other phosphodiesterases. PDM-042 can be used for the research of schizophrenia.
    PDM-042
  • HY-155692
    PDE4-IN-13
    		Inhibitor
    PDE4-IN-13 is a PDE4 inhibitor with an IC50 of 1.56 μM. PDE4-IN-13 shows anti-inflammatory and antioxidant properties， and can be used for chronic obstructive pulmonary disease (COPD) research.
    PDE4-IN-13
  • HY-163777
    Talaroterphenyl A
    		Inhibitor
    Talaroterphenyl A (compound 1) is a p-terphenyl derivative present in the mangrove sediment-derived fungus Talaromyces sp. SCSIO 41412, which exhibits phosphodiesterase 4 (PDE4) inhibitory activity (IC50=1.2 μM). Talaroterphenyl A also exhibits anti-inflammatory and anti-fibrotic activities, significantly reducing the mRNA levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β.
    Talaroterphenyl A
  • HY-10568
    TC-E 5005
    		Inhibitor
    TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate.
    TC-E 5005
  • HY-124388
    PDE4-IN-20
    PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors.
    PDE4-IN-20
  • HY-117715
    CK-3197
    		Inhibitor
    CK-3197 is a weak inhibitor of Peak lll cyclic 3'5'-adenosine monophosphate phosphodiesterase (CAMP PDEl). CK-3197 has hemodynamic and myocardial energetic effects in vivo. CK-3197 is an imidazolone derivative used as a selective positive inotropic agent for congestive heart failure.
    CK-3197
  • HY-RS10207
    Pde12 Rat Pre-designed siRNA Set A
    		Inhibitor

    Pde12 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pde12 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Pde12 Rat Pre-designed siRNA Set A
    Pde12 Rat Pre-designed siRNA Set A
  • HY-176409
    Phosphodiesterase-IN-4
    		Inhibitor
    Phosphodiesterase-IN-4 (compound 18) is a potent Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor. Phosphodiesterase-IN-4 inhibits colorectal cancer cells with an IC50 of 6.9 μM.
    Phosphodiesterase-IN-4
  • HY-146201
    PDE4B/7A-IN-1
    PDE4B/7A-IN-1 (compound 7) is a PDE4B/PDE7A inhibitor (PDE4B, IC50=80.4 μM) and 5-HT1A/5-HT-7R antagonist. PDE4B/7A-IN-1 has membrane-penetrating activity and high metabolic stability. PDE4B/7A-IN-1 exhibits antidepressant properties in rat behavioral tests.
    PDE4B/7A-IN-1
  • HY-147846
    AChE/PDE4-IN-1
    		Inhibitor
    AChE/PDE4-IN-1 (compound 12c) is a potent and selective dual PDE4/AChE inhibitor, with IC50s of 0.28 μM and 1.88 μM for AChE and PDE4D, respectively. AChE/PDE4-IN-1 exhibits anti-neuroinflammatory effect for the research of Alzheimer's disease.
    AChE/PDE4-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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