Phosphodiesterase (PDE)
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
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Phosphodiesterase (PDE)
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PDE1
(60)
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PDE2
(51)
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PDE3
(93)
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PDE4
(198)
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PDE5
(97)
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PDE6
(22)
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PDE7
(28)
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PDE9
(19)
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PDE10
(53)
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PDE11
(13)
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PDE12
(2)
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PDE8
(11)
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Autotaxin
(36)
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All Product Categories
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Phosphodiesterase (PDE) Inhibitors
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Phosphodiesterase (PDE) Agonists
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Phosphodiesterase (PDE) Antagonists
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Phosphodiesterase (PDE) Activators
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Phosphodiesterase (PDE) Modulators
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Phosphodiesterase (PDE) Degraders
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Phosphodiesterase (PDE) Controls
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Phosphodiesterase (PDE) Substrates
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Phosphodiesterase (PDE) Ligand
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Phosphodiesterase (PDE) Related Products (1009)
Related Products (1009)
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Antibodies (4)
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Phosphodiesterase (PDE) Isoform Comparison
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BAY 2666605
0 ImagesBAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135).
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Trequinsin hydrochloride
0 ImagesSynonyms: HL 725Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia).
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Carbazeran
0 ImagesCarbazeran is a phosphodiesterase inhibitor. Carbazeran is oxidized by aldehyde oxidase/AOX1 to 4-oxo-carbazeran/hydroxycarbazeran, serving as an AOX1 probe and competitively inhibiting xanthine oxidase. Carbazeran can be used in research on congestive heart failure and chronic heart failure.
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PDE4B-IN-2
0 ImagesPDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 μM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.
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Eurycomanone
0 ImagesSynonyms: Pasakbumin AEurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
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Vardenafil hydrochloride
0 ImagesVardenafil 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].
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Enpp-1-IN-14
0 ImagesEnpp-1-IN-14 (Compound 015) is a potent Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) inhibitor with an IC50 value of 32.38 nM for recombinant human ENPP-1. Enpp-1-IN-14 has anti-tumor activity.
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Edelinontrine
0 ImagesSynonyms: PF-04447943Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM).
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Elpipodect
0 ImagesSynonyms: MK-8189Elpipodect (MK-8189) is an orally active and selective PDE10A inhibitor with a Ki value of 29 pM. Elpipodect can be used in research of schizophrenia.
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Fraxin
0 ImagesFraxin isolated from Cortex Fraxini, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
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Fenspiride hydrochloride
0 ImagesFenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
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GSK256066
0 ImagesGSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.
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Glaucine
0 ImagesSynonyms: O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer.
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Roflumilast N-oxide
0 ImagesRoflumilast N-oxide is a PDE type 4 inhibitor.
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YM976
0 ImagesYM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses.
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BAY 73-6691
0 ImagesBAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
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Deltarasin
0 ImagesDeltarasin is an inhibitor of?KRAS-PDEδ interaction with?Kd?of 38 nM for binding to purified PDEδ.
