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-112555
    PDE7-IN-2
    		Inhibitor ≥99.0%
    PDE7-IN-2 (compound 2) is a potent PDE7 (phosphodiesterase 7) inhibitor with IC50 value of 2.1 µM. PDE7-IN-2 has the potential for the research of parkinson’s disease.
    PDE7-IN-2
  • HY-W177546
    CD00509
    		Inhibitor 98.0%
    CD00509 is a tyrosyl-DNA phosphodiesterase (PDE) Tdp1 inhibitor with an IC50 of 0.71 μM. CD00509 increases DNA damage and promotes apoptosis of MCF-7 cells. CD00509 can sensitize breast cancer cells and wild-type murine embryonic fibroblasts (MEFs) to Camptothecin (CPT) (HY-16560). CD00509 can be used for the study of cancers such as breast cancer.
    CD00509
  • HY-14464
    PF-00489791
    		Inhibitor 99.70%
    PF-00489791 (PF-489791) is a potent inhibitor of phosphodiesterase 5A with IC50 of 1.5 nM. PF-00489791 can enhance the relaxation of blood vessels within the kidney and so reduce blood pressure, improving renal function.
    PF-00489791
  • HY-142059
    PDE5-IN-4
    		Inhibitor 99.60%
    PDE5-IN-4 is a phosphodiesterase 5 inhibitor. PDE5-IN-4 can be used for the research of acute myocardial infarction and damage caused by reperfusion, gastrointestinal diseases, damage caused by diabetes, and liver failure.
    PDE5-IN-4
  • HY-164368
    GLUT4 activator 2
    		Activator
    GLUT4 activator 2 (C59) is an insulin sensitizer, which can be used for research of diabetic diseases. GLUT4 activator 2 improves glucose uptake and insulin sensitivity in rodents. GLUT4 activator 2 interacts with Unc119 and Unc119B resulting in increased insulin sensitivity and GLUT4 translocation.
    GLUT4 activator 2
  • HY-100326
    PDE7-IN-3
    		Inhibitor 99.94%
    Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain.
    PDE7-IN-3
  • HY-14252A
    Milrinone lactate
    		Inhibitor 98.76%
    Milrinone lactate is a potent inotropic dilating agent. Milrinone lactate shows simultaneous positive inotropic and vasodilating activities. Milrinone lactate promotes reduction of SVR and PVR in patients with DCM and NYHA class III and IV of heart failure. Milrinone lactate has the potential for the research of cardiovascular function after cardiac surgery and in septic shock.
    Milrinone lactate
  • HY-N7272
    Cirsimarin
    		Inhibitor 99.95%
    Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase.
    Cirsimarin
  • HY-157886
    TDP1 Inhibitor-3
    		Inhibitor 98.10%
    TDP1 Inhibitor-3 (Compound 4E) is a (TDP1) inhibitor with an IC50 value of 0.63 μM.
    TDP1 Inhibitor-3
  • HY-B1209
    Etofylline
    		Inhibitor 99.72%
    Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos.
    Etofylline
  • HY-145561
    Cudetaxestat
    		Inhibitor 98.32%
    Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc.
    Cudetaxestat
  • 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-111410
    ATX inhibitor 1
    		Inhibitor 99.30%
    ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
    ATX inhibitor 1
  • HY-12740
    Lotamilast
    		Inhibitor 98.0%
    Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
    Lotamilast
  • HY-109193
    Tovinontrine
    		Inhibitor 99.83%
    Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.
    Tovinontrine
  • HY-128593
    TPN171
    		Inhibitor 98.10%
    TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH).
    TPN171
  • HY-124768
    PDE12-IN-3
    		Inhibitor 98.02%
    PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity.
    PDE12-IN-3
  • HY-12812
    Autotaxin modulator 1
    		Modulator 99.40%
    Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.
    Autotaxin modulator 1
  • HY-147263
    Dovramilast
    		Inhibitor 99.66%
    Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (HY-B0329)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB).
    Dovramilast
  • HY-106003
    GSK356278
    		Inhibitor 99.82%
    GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.
    GSK356278
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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