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-W177546
    CD00509
    		Inhibitor ≥98.0%
    CD00509 is a Tdp1 inhibitor, with an IC50 value of 0.71 μM. CD00509 can sensitize breast cancer cells to Camptothecin (HY-16560). CD00509 has anti-tumor activity.
    CD00509
  • HY-14464
    PF-00489791
    		Inhibitor 99.70%
    PF-00489791 (PF-489791) is a potent inhibitor of phosphodiesterase 5A with IC50 of 1.5 nM. PF-00489791 can enhance the relaxation of blood vessels within the kidney and so reduce blood pressure, improving renal function.
    PF-00489791
  • HY-119611A
    Thioquinapiperifil dihydrochloride
    		Inhibitor 99.22%
    Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.
    Thioquinapiperifil dihydrochloride
  • HY-50098A
    Mardepodect hydrochloride
    		Inhibitor 99.94%
    Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
    Mardepodect hydrochloride
  • HY-B0004S
    Doxofylline-d6
    		Inhibitor ≥99.0%
    Doxofylline-d6 is the deuterium labeled Doxofylline. Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
    Doxofylline-d<sub>6</sub>
  • HY-108619
    Gisadenafil besylate
    		Inhibitor ≥99.0%
    Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
    Gisadenafil besylate
  • HY-13344A
    PF-8380 hydrochloride
    		Inhibitor 98.59%
    PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380 hydrochloride
  • HY-19830
    AN3199
    		Inhibitor 99.76%
    AN3199 is a PDE4 inhibitor with an IC50 of 94.5 nM. AN3199 can be used for the research of inflammation-associated diseases such as asthma and chronic obstructive pulmonary disease (COPD).
    AN3199
  • HY-B0523
    Anagrelide
    		Inhibitor 99.87%
    Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide
  • HY-111410
    ATX inhibitor 1
    		Inhibitor 99.30%
    ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
    ATX inhibitor 1
  • HY-153192A
    Nerandomilast dihydrate
    		Inhibitor 99.93%
    Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).
    Nerandomilast dihydrate
  • HY-124768
    PDE12-IN-3
    		Inhibitor 98.02%
    PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity.
    PDE12-IN-3
  • HY-131707
    LEO 39652
    		Inhibitor 99.51%
    LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
    LEO 39652
  • HY-147263
    Dovramilast
    		Inhibitor 99.83%
    Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB).
    Dovramilast
  • HY-117318
    PDE12-IN-1
    		Inhibitor 98.85%
    PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.
    PDE12-IN-1
  • HY-135490
    Reproterol
    		Inhibitor
    Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research.
    Reproterol
  • HY-163343
    Enpp-1-IN-20
    		Inhibitor 98.06%
    Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer.
    Enpp-1-IN-20
  • HY-106045
    Imazodan
    		Inhibitor 99.38%
    Imazodan is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan serves also as a peripheral vasodilator.
    Imazodan
  • HY-135848
    N-Methylbenzamide
    		Inhibitor 99.93%
    N-Methylbenzamide is a potent phosphodiesterase 10A (PDE10A) inhibitor. N-Methylbenzamide has anti-cancer activity.
    N-Methylbenzamide
  • HY-106739
    Motapizone
    		Inhibitor
    Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP.
    Motapizone
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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