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-103160A
    EHNA hydrochloride
    		Inhibitor 99.61%
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects.
    EHNA hydrochloride
  • HY-100912
    W-7 hydrochloride
    		Inhibitor 99.65%
    W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.
    W-7 hydrochloride
  • HY-13344
    PF-8380
    		Inhibitor 99.04%
    PF-8380 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
  • HY-B0715
    Pentoxifylline
    		Inhibitor 99.92%
    Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
    Pentoxifylline
  • HY-10978
    Crisaborole
    		Inhibitor
    Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
    Crisaborole
  • HY-15025A
    Sildenafil citrate
    		Inhibitor 99.73%
    Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate
  • HY-B0763
    Ibudilast
    		Inhibitor 99.89%
    Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
    Ibudilast
  • HY-14992
    Bay 60-7550
    		Inhibitor 98.14%
    Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM.
    Bay 60-7550
  • HY-B0764A
    Bucladesine calcium
    		Inhibitor 99.52%
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
    Bucladesine calcium
  • HY-B1816
    Zaprinast
    		Inhibitor 99.95%
    Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
    Zaprinast
  • HY-15441
    Edelinontrine
    		Inhibitor 98.74%
    Edelinontrine (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).
    Edelinontrine
  • HY-16558
    Butein
    		Inhibitor 99.95%
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein
  • HY-129490
    Enpp-1-IN-1
    		Inhibitor 99.86%
    Enpp-1-IN-1 is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor extracted from patent WO2019046778, Example 55.
    Enpp-1-IN-1
  • HY-15426
    PF-04957325
    		Inhibitor 98.89%
    PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
    PF-04957325
  • HY-13295
    Vinpocetine
    		Inhibitor 99.57%
    Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
    Vinpocetine
  • HY-W028690
    DNMDP
    		Inhibitor 98.95%
    DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
    DNMDP
  • HY-122942
    Moracin M
    		Inhibitor 98.90%
    Moracin M is a phenolic component that can be isolated from Mori Cortex, is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity.
    Moracin M
  • HY-145319
    FPFT-2216
    		Inhibitor 99.35%
    FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.
    FPFT-2216
  • HY-18252
    Avanafil
    		Inhibitor ≥98.0%
    Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
    Avanafil
  • HY-B0523A
    Anagrelide hydrochloride
    		Inhibitor 99.66%
    Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide hydrochloride
Phosphodiesterase (PDE) Isoform Comparison

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