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-116755
    Tiropramide
    		Inhibitor
    Tiropramide (CR 605) is a tyrosine derivative with antispastic properties. Tiropramide hydrochloride inhibits phosphodiesterase activity involved in cAMP catabolism in rabbit colon homogenates. Tiropramide relaxes smooth muscle in rabbit isolated colon. Tiropramide can be used for the research of irritable colon and biliary dyskinesia.
    Tiropramide
  • HY-120291
    ASP9436
    		Inhibitor
    ASP9436 is an orally active and blood-brain barrier permeable PDE10A inhibitor with an IC50 of 8 nM against human PDE10A. ASP9436 attenuates locomotor activity in mouse hyperactivity models and ameliorates visual recognition memory impairment in neonatal mice. ASP9436 is applicable to research related to schizophrenia.
    ASP9436
  • HY-B0523AR
    Anagrelide hydrochloride (Standard)
    		Inhibitor
    Anagrelide (hydrochloride) (Standard) is the analytical standard of Anagrelide (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-106137
    Tofimilast
    		Inhibitor
    Tofimilast is an inhibitor of Phosphodiesterase 4 (PDE4) with an IC50 of 0.14 μM. Tofimilast exerts its anti-inflammatory effects by inhibiting the activity of PDE4, thereby increasing intracellular levels of cAMP.
    Tofimilast
  • HY-14930R
    Mirodenafil (Standard)
    		Inhibitor
    Mirodenafil (Standard) is the analytical standard of Mirodenafil. This product is intended for research and analytical applications. Mirodenafil (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).
    Mirodenafil (Standard)
  • HY-146123
    ATX inhibitor 20
    		Inhibitor
    ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.3 nM.
    ATX inhibitor 20
  • HY-169071S
    ATX-1905
    		Inhibitor
    ATX-1905 is a positron emission tomography (PET) tracer that demonstrates good autotaxin (ATX) binding specificity and achieves semiquantification of lung ATX expression levels, which are elevated in fibrotic lungs. ATX-1905 exhibits elevated uptake in Bleomycin (HY-108345)-induced pulmonary fibrosis (BPF) lungs. ATX-1905 is promising for research of idiopathic pulmonary fibrosis (IPF).
    ATX-1905
  • HY-B0809S1
    Theophylline-d3
    		Inhibitor
    Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline-d<sub>3</sub>
  • HY-182415
    RX-RA-69
    		Inhibitor
    RX-RA-69 is an orally active platelet phosphodiesterase (PDE) inhibitor with a IC50 of 1 nM. RX-RA-69 elevates cAMP levels in platelets, exerts anti-aggregatory effects, and inhibits the formation of coronary platelet thrombi. RX-RA-69 exhibits anti-metastatic activity in a mouse Lewis lung cancer model. RX-RA-69 can be used in research related to coronary platelet thrombi and Lewis lung cancer.
    RX-RA-69
  • HY-179337
    PDE2-IN-1
    		Inhibitor
    PDE2-IN-1 is a potent and orally active PDE2 inhibitor with an IC50 of 0.6 μM, demonstrating neuroprotective effects. PDE2-IN-1 modulates the PKA/CREB/BDNF signaling pathway by inhibiting PDE2. PDE2-IN-1 improves memory deficits and cognitive impairment in an okadai acid (OKA)-induced Alzheimer’s disease (AD) mouse model. PDE2-IN-1 can be used for the research of AD.
    PDE2-IN-1
  • HY-19003A
    Isomazole hydrochloride
    		Inhibitor
    Isomazole (323MHb) hydrochloride is a cardiotonic agent. Isomazole hydrochloridei increases the calcium sensitivity in atrial fibers and has a direct effect on contractile proteins.
    Isomazole hydrochloride
  • HY-111167
    AN-2898
    		Inhibitor
    AN-2898 is a selective PDE4 inhibitor with IC50 of 0.027 μM over other phosphodiesterase enzymes, such as PDE1A, PDE2A and PDE3A. AN-2898 also potently inhibits PDE4 subtypes (PDE4B1, PDE4A1A and PDE4D2). AN-2898 significantly inhibits the production of TNF-α, IL-2, IFN-γ, IL-5 and IL-10. AN-2898 can be used for mild to moderate atopic dermatitis (AD) and psoriasis research.
    AN-2898
  • HY-129210
    KMUP-4
    		Inhibitor
    KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K+ channels. KMUP-4 can be used in the study of cardiovascular diseases.
    KMUP-4
  • HY-121041
    GEBR-7b
    GEBR-7b is a selective PDE4D inhibitor with an IC50 of 0.67 μM. GEBR-7b increases hippocampal cAMP and does not influence Aβ levels in rodents. GEBR-7b also improves spatial and can be used for the study of cognitive deficits.
    GEBR-7b
  • HY-121421
    Diniprofylline
    		Inhibitor
    Diniprofylline, a bronchodilator, is a phosphodiesterase inhibitor. Diniprofylline possesses the potential to interact with human ACE2 and prevent its recognition by SARS-CoV-2.
    Diniprofylline
  • HY-143420
    ATX inhibitor 15
    		Inhibitor
    ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
    ATX inhibitor 15
  • HY-19089
    DPN-205-734
    		Inhibitor
    DPN-205-734 is an orally administered cGMP-PDE inhibitor. DPN-205-734 exhibits positive inotropic effects in various animal cardiomyocytes. DPN-205-734 reduces blood pressure and total peripheral resistance in multiple animal models, demonstrating a debulking effect. DPN-205-734 can be used in research on cardiovascular and cerebrovascular diseases such as heart failure.
    DPN-205-734
  • HY-147991
    PDE5/HDAC-IN-1
    		Inhibitor
    PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.
    PDE5/HDAC-IN-1
  • HY-175779
    TDP1-IN-4
    		Inhibitor
    TDP1-IN-4 (Compound 33) is a Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 0.90  μM. TDP1-IN-4 has a strong synergistic effect with Camptothecin (HY-16560) in SK-Mel-2 cells, but not in cancer cells (A549, HCT-116 and MCF-7 cells) and non-cancerous Ges-1 cells. TDP1-IN-4 can be used for cancer chemotherapy and radiotherapy research.
    TDP1-IN-4
  • HY-N3180
    Norbraylin
    		Inhibitor
    Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM.
    Norbraylin
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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