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-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 (Compound G1) 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-14826
    Tilivapram
    		Inhibitor 99.96%
    Tilivapram (AVE8112) is an orally active PDE4 inhibitor. Tilivapram can regulate neurophysiological activities and improve cognitive and memory impairments. Tilivapram can be used in the research of various neuropsychiatric disorders such as schizophrenia and Parkinson's disease.
    Tilivapram
  • 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
  • HY-160991A
    Menabitan dihydrochloride
    		Inhibitor
    Menabitan dihydrochloride (SP-204 dihydrochloride) is the dihydrochloride form of Menabitan (HY-160991). Menabitan dihydrochloride is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan dihydrochloride lowers the intraocular pressure in rabbit model.
    Menabitan dihydrochloride
  • HY-177077
    Davalomilast
    		Inhibitor
    Davalomilast (Example 100) is an PDE4 inhibitor with anti-inflammatory property. Davalomilast can be studied in research for autoimmune diseases and dermatology research.
    Davalomilast
  • HY-172365
    P7–2302
    		Inhibitor
    P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F.
    P7–2302
  • HY-152838
    Gemlapodect
    		Inhibitor
    Gemlapodect (RO554965) is an inhibitor of phosphodiesterase 10A (PDE10A). Gemlapodect can be used for researching schizophrenia.
    Gemlapodect
  • HY-153802A
    Antitumor agent-100 hydrochloride
    Antitumor agent-100 (compound A6) hydrochloride is an orally potent apoptosis inducer and molecular gel targeting PDE3A-SLFN12 (IC50: 0.3 μM) with antitumor activity. Antitumor agent-100 hydrochloride binds to the PDE3A enzyme pocket to recruit and stabilize SLFN12, thereby preventing protein translation and leading to apoptosis.
    Antitumor agent-100 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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