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-100438
    Hydronidone
    		Inhibitor 99.92%
    Hydronidone is an orally active pyridine derivative. Hydronidone is an inhibitor of phosphodiesterase-4 (PDE4) and cyclo-oxygenase (COX) as well as TGF-β. Hydronidone induces mitochondrial dysfunction and triggers apoptosis. Hydronidone can be used for liver fibrosis, anti-inflammation and anti-cancer study.
    Hydronidone
  • HY-122751
    (R)-DNMDP
    		Inhibitor 99.59%
    (R)-DNMDP is a potent and selective cancer cell cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, binds PDE3A directly. (R)-DNMDP has a 500-fold lower EC50 compared to the (S)-enantiomer in HeLa cell line.
    (R)-DNMDP
  • HY-139362
    Enpp-1-IN-2
    		Inhibitor 99.16%
    Enpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe.
    Enpp-1-IN-2
  • HY-136637
    NPD-001
    		Inhibitor 99.50%
    NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM.
    NPD-001
  • HY-119372
    TDP1 Inhibitor-1
    		Inhibitor 98.33%
    TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM.
    TDP1 Inhibitor-1
  • 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-136350
    BRD9500
    		Modulator 99.46%
    BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
    BRD9500
  • HY-128879A
    VP3.15 dihydrobromide
    		Inhibitor 98.01%
    VP3.15 dihydrobromide 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 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
    VP3.15 dihydrobromide
  • HY-108974
    Drotaverine hydrochloride
    		Inhibitor 99.65%
    Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
    Drotaverine hydrochloride
  • HY-P1077A
    CALP1 TFA
    		Activator 99.86%
    CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
    CALP1 TFA
  • HY-153335
    Enpp-1-IN-16
    		Inhibitor 99.11%
    Enpp-1-IN-16 (compound 54) is an ENPP1 inhibitor. Enpp-1-IN-16 has the potential to study cancer, especially in cases of high ENPP1 expression or elevated cytoplasmic DNA levels. Enpp-1-IN-16 can also be used in other diseases mediated by ENPP1, such as bacterial or viral infections, insulin resistance and type II diabetes, chondrocalcinosis and osteoarthritis, calcium pyrophosphate deposition disorder (CPPD), low Phosphatase disease and soft tissue calcification disorders.
    Enpp-1-IN-16
  • HY-B1639
    Enoximone
    		Inhibitor 99.91%
    Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
    Enoximone
  • HY-N1860
    3-O-Methylquercetin
    		Inhibitor 99.98%
    3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma.
    3-O-Methylquercetin
  • HY-B1294
    Amrinone
    		Inhibitor 98.04%
    Amrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
    Amrinone
  • HY-100936
    Etazolate hydrochloride
    		Inhibitor 98.00%
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
    Etazolate hydrochloride
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone
    		Inhibitor 99.86%
    3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma.
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone
  • HY-B0327
    Irsogladine
    		Inhibitor 99.97%
    Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.
    Irsogladine
  • HY-136569
    DSR-141562
    		Inhibitor 99.98%
    DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
    DSR-141562
  • HY-112831
    Osoresnontrine
    		Inhibitor 99.88%
    Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.
    Osoresnontrine
  • HY-N6781
    Ophiobolin A
    		Inhibitor 99.53%
    Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
    Ophiobolin A
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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