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-100650
    Carbodenafil
    		Inhibitor 99.63%
    Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
    Carbodenafil
  • HY-100530B
    Sp-cAMPS
    		Inhibitor
    Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
    Sp-cAMPS
  • HY-155830
    Morcamilast
    		Inhibitor 98.92%
    Morcamilast (ME3183) is a selective and orally active PDE4 inhibitor, with IC50s of 1.28 nM (PDE4A1A), 2.33 nM (PDE4B1), and 1.63 nM (PDE4D2) respectively. Morcamilast shows weak inhibition of PDEs other than PDE4s Morcamilast is an anti-inflammatory agent and inhibits LPS (HY-D1056)-induced release of TNF-α, IL-12/23p40, IL-23, and IL-17A in human PBMCs and T cells. Morcamilast has antipruritic effect and can be used in the study of psoriasis, atopic dermatitis, and other inflammatory diseases.
    Morcamilast
  • HY-169402
    PDE1-IN-9
    		Inhibitor
    PDE1-IN-9 (Compound 7a) is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 exhibits good metabolic stability in rat liver microsomes.
    PDE1-IN-9
  • HY-116100A
    HA155
    		Inhibitor 98.00%
    HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.
    HA155
  • HY-18078
    PQ-10
    		Inhibitor 99.77%
    PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia.
    PQ-10
  • HY-B0715S2
    Pentoxifylline-d5
    		Inhibitor 99.89%
    Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. 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-d<sub>5</sub>
  • HY-136350B
    (S)-BRD9500
    		Control 99.67%
    (S)-BRD9500 is the isomer of BRD9500 (HY-136350), and can be used as an experimental control. BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
    (S)-BRD9500
  • HY-19026
    Siguazodan
    		Inhibitor 99.06%
    Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
    Siguazodan
  • HY-101803
    CP671305
    		Inhibitor 99.95%
    CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
    CP671305
  • HY-100615
    Revizinone
    		Inhibitor 99.75%
    Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.
    Revizinone
  • HY-15025S2
    Sildenafil-d3N-1
    		99.47%
    Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
    Sildenafil-d<sub>3</sub>N<sub>-1
  • HY-103267
    S32826 disodium
    		Inhibitor 98.85%
    S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes.
    S32826 disodium
  • HY-169402A
    PDE1-IN-9 hydrochloride
    		Inhibitor
    PDE1-IN-9 (Compound 7a) hydrochloride is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC50 of 11 nM. PDE1-IN-9 hydrochloride reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 hydrochloride exhibits good metabolic stability in rat liver microsomes.
    PDE1-IN-9 hydrochloride
  • HY-15747A
    Deltarasin hydrochloride
    		Inhibitor 98.07%
    Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.
    Deltarasin hydrochloride
  • HY-A0165
    Tofisopam
    		Inhibitor 99.46%
    Tofisopam, a 2,3-benzodiazepine compound, is an orally active anxiolytic agent. Tofisopam can inhibit phosphodiesterase PDE isoenzyme activity, withIC50 values of 2.11 μM, 1.98 μM, 0.42 μM, and 0.92 μM for PDE-2A3, PDE-3A, PDE-4A1, and PDE-10A1, respectively. Tofisopam can be used for the study of anxiety.
    Tofisopam
  • HY-115555
    K-Ras-PDEδ-IN-1
    		Inhibitor 99.62%
    K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM.
    K-Ras-PDEδ-IN-1
  • HY-12913
    AMG 579
    		Inhibitor 99.02%
    AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.
    AMG 579
  • HY-B0312S
    Dipyridamole-d20
    		Inhibitor ≥98.0%
    Dipyridamole-d20 is the deuterium labeled Dipyridamole. Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.
    Dipyridamole-d<sub>20</sub>
  • HY-131973
    PDE10A-IN-2 hydrochloride
    		Inhibitor 98.43%
    PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
    PDE10A-IN-2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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