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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Etazolate hydrochloride
0 ImagesSynonyms: SQ 20009; EHT 0202 hydrochlorideEtazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
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OPB-171775
0 ImagesOPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.
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Sildenafil-d3
0 ImagesSynonyms: UK-92480-d3Sildenafil-d3 is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
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Enpp-1-IN-12
0 ImagesEnpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.
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Enpp-1-IN-2
0 ImagesEnpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe.
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D(+)-Raffinose pentahydrate
0 ImagesSynonyms: D-Raffinose pentahydrateD(+)-Raffinose pentahydrate is an orally active inhibitor of LecA (Kd = 32 μM) and GtfC. D(+)-Raffinose pentahydrate reduces cyclic diguanylate (c-di-GMP) by increased activity of a c-di-GMP specific phosphodiesterase. D(+)-Raffinose pentahydrate interferes with GTF function. D(+)-Raffinose pentahydrate decreases IL-4 and IL-5 mRNA. D(+)-Raffinose pentahydrate exhibits biofilm-inhibitory activity against Pseudomonas aeruginosa and Streptococcus mutans and inhibits allergic airway eosinophilia.
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NPD-001
0 ImagesNPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection.
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DSR-141562
0 ImagesDSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
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TDP1 Inhibitor-1
0 ImagesTDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM. TDP1 Inhibitor-1 shows cytotoxicity against multiple cancer cells. TDP1 Inhibitor-1 can be used for the research of cancer, such as breast cancer.
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Amrinone
0 ImagesSynonyms: InamrinoneAmrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
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Zardaverine
0 ImagesZardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
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Mufemilast
0 ImagesSynonyms: Hemay005Mufemilast (Heymay005) is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor (IC50 = 80-120 nM). Mufemilast modulates cytokines upregulated in Behςet’s syndrome (BS). Mufemilast displays a significant inhibitory effect on TNF-α, which is an important proinflammatory cytokine target in the disease process of psoriasis. Mufemilast can be studied in research for diseases such as rheumatoid arthritis, psoriasis and BS.
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Linderane
0 ImagesLinderane is an orally active natural sesquiterpene lactone with blood-brain barrier permeability. Linderane indirectly activates PDE3 by activating ERK/STAT3, thereby inhibiting the cAMP/PKA/CREB signaling pathway and hepatic gluconeogenesis. Linderane protects pancreatic β cells against oxidative damage by inhibiting the activation of the p38 MAPK pathway and activating the Nrf2 pathway. Linderane inhibits cell apoptosis and ameliorates intestinal mucosal inflammation by suppressing the IL-6/JAK/STAT3 signaling pathway. Linderane reduces pain sensitivity and alleviates anxiety-like behaviors by activating cannabinoid receptor 2 (CB2R). Linderane can be used in studies related to type 2 diabetes, ulcerative colitis, and chronic inflammatory pain with anxiety.
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STF-1084
0 ImagesSTF-1084 is a specific, cell-impermeable, competitive inhibitor of ENPP1 (Ki = 33 nM). STF-1084 increases extracellular cGAMP concentrations by preventing its degradation by ENPP1, thereby enhancing immune infiltration. STF-1084 acts synergistically with ionizing radiation (IR) and cGAMP to delay tumor progression. STF-1084 can be used to study cancers with low immunogenicity.
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Ethaverine hydrochloride
0 ImagesEthaverine hydrochloride is a Papaverine derivative and vasodilator. Ethaverine hydrochloride inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrochloride blocks L-type Ca2+ channels, reduces intracellular Ca2+ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrochloride alters cochlear microcirculation, intracochlear Po2, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrochloride is used in the research of peripheral vascular diseases.
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Mirodenafil
0 ImagesSynonyms: SK3530Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
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Sp-cAMPS sodium salt
0 ImagesSp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
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Phyllodulcin
0 ImagesPhyllodulcin is an orally active sweetener found in Hydrangea macrophylla var. thunbergii. Phyllodulcin acts as a non-selective phosphodiesterase inhibitor and exerts anti-allergic effects by suppressing lymphocyte activation. Phyllodulcin can be used to combat obesity by regulating levels of leptin, fat browning-related genes, and hypothalamic BDNF-TrkB signaling.
