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-128879
    VP3.15
    		Inhibitor
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
    VP3.15
  • HY-B0809A
    Theophylline monohydrate
    Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline monohydrate
  • HY-106358A
    Andolast
    		Inhibitor
    Andolast (CR 2039) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma.
    Andolast
  • HY-130262
    PDE1-IN-3
    		Inhibitor
    PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1 (PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively.
    PDE1-IN-3
  • HY-128349
    MT-3014
    		Inhibitor
    MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively.
    MT-3014
  • HY-17464S
    Cilostazol-d11
    		Inhibitor
    Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.
    Cilostazol-d<sub>11</sub>
  • HY-15455S1
    Roflumilast-d4 N-Oxide
    		Inhibitor 98.13%
    Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
    Roflumilast-d<sub>4</sub> N-Oxide
  • HY-131101S
    Nor-Acetildenafil-d8
    Nor-Acetildenafil-d8 is the deuterium labeled Nor-Acetildenafil. Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
    Nor-Acetildenafil-d8
  • HY-13927S
    Acetildenafil-d8
    Acetildenafil-d8 is the deuterium labeled Acetildenafil. Acetildenafil is a derivative of the phosphodiesterase 5 (PDE5) inhibitor Sildenafil.
    Acetildenafil-d<sub>8</sub>
  • HY-15025S1
    Sildenafil-d8
    		Inhibitor
    Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
    Sildenafil-d<sub>8</sub>
  • HY-18253S
    Udenafil-d7
    		Inhibitor
    Udenafil-d7 is the deuterium labeled Udenafil. Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
    Udenafil-d<sub>7</sub>
  • HY-176234
    PDE4-IN-28
    		Inhibitor
    PDE4-IN-28 is a PDE4D inhibitor (IC50: 29 nM). PDE4-IN-28 inhibits the production of TNF-α and NO (IC50: 13.32 and 2.32 μM, respectively). PDE4-IN-28 exhibits anti-inflammatory, antibacterial and analgesic effects in a rat pressure ulcer (PU) model and promotes HUVEC cell migration, thereby accelerating wound healing.
    PDE4-IN-28
  • HY-173640
    ID11916
    		Inhibitor
    ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3.
    ID11916
  • HY-110005
    Sp-cAMPS triethylamine
    		Inhibitor
    Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM.
    Sp-cAMPS triethylamine
  • HY-162912
    Enpp-1-IN-23
    		Inhibitor
    Enpp-1-IN-23 (compound 27) is an Enpp-1 inhibitor, with IC50 of 1.2 nM. Enpp-1-IN-23 can be used in cancer research.
    Enpp-1-IN-23
  • HY-126812
    Longestin
    		Inhibitor
    Longestin (KS-505a) is a specific inhibitor of phosphodiesterase with antitrypanosomal activity, which is derived from Streptomyces argenteolus. Longestin is promising for research of anti-amnesia agent.
    Longestin
  • HY-16558R
    Butein (Standard)
    		Inhibitor
    Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. 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 (Standard)
  • HY-168491
    Enpp-1-IN-25
    		Inhibitor
    Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy.
    Enpp-1-IN-25
  • HY-173360
    PDE10A-IN-5
    		Inhibitor
    PDE10A-IN-5 (Compound A30) is an inhibitor of phosphodiesterase 10A (PDE10A) with oral activity, and its IC50 value is 3.5 nM. PDE10A-IN-5 exerts the activity of inhibiting pulmonary vascular remodeling by inhibiting PDE10A and activating the cyclic adenosine monophosphate (cAMP)-associated signaling pathway, and can be used for research in the field of pulmonary arterial hypertension.
    PDE10A-IN-5
  • HY-120241
    Reticulol
    		Inhibitor
    Reticulol (K 251-1) is an inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase. Reticulol shows antitumor activity independent with cell cycle arrest or apoptosis. Reticulol inhibits cell growth of murine melanoma cells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma.
    Reticulol
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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