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. 상품명 효과 Purity Chemical Structure
  • 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-18740
    Trequinsin
    		Inhibitor
    Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia).
    Trequinsin
  • HY-181589
    PDE11A4-IN-2
    		Inhibitor
    PDE11A4-IN-2 is a selective PDE11A4 inhibitor with an IC50 of 33 nM. PDE11A4-IN-2 functionally inhibits PDE11A4-mediated catalytic activities of cAMP and cGMP in cellular models. PDE11A4-IN-2 is applicable to the research of age-related cognitive decline.
    PDE11A4-IN-2
  • 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-112631
    OPC 33540
    		Inhibitor
    OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC50 values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC50s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.
    OPC 33540
  • 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
  • HY-147998
    Enpp-1-IN-13
    		Inhibitor
    Enpp-1-IN-13 (Compound 1a) is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor with IC50 values of 1.29 μM and 20.2 μM against ENPP1 and ENPP3, respectively. Enpp-1-IN-13 shows anticancer activity.
    Enpp-1-IN-13
  • HY-183546
    TDP1-IN-6
    		Inhibitor
    TDP1-IN-6 is a TDP1 inhibitor with an IC50 of 1.52 μM. Combination of TDP1-IN-6 with Topotecan (HY-13768) enhances DNA damage, induces Apoptosis, triggers S-phase cell cycle arrest, and promotes Ferroptosis. TDP1-IN-6 can be used for the research of cervical cancer.
    TDP1-IN-6
  • HY-17464S1
    Cilostazol-d4
    		Inhibitor
    Cilostazol-d4 is 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>4</sub>
  • HY-120997
    E6 Berbamine
    		Inhibitor
    E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activities of calmodulin-dependent myosin light chain kinase (MLCK) and phosphodiesterase (PDE). E6 Berbamine exhibits anti-leukemic activity. E6 Berbamine can be used in research related to cardiovascular abnormalities and chronic myeloid leukemia.
    E6 Berbamine
  • HY-128234
    PDE11-IN-1
    		Inhibitor 98.23%
    PDE11-IN-1 is a PDE11 inhibitor and can be used for adrenal insufficiency research.
    PDE11-IN-1
  • HY-172919
    PDEδ/NAMPT IN-1
    		Inhibitor
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD+), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer.
    PDEδ/NAMPT IN-1
  • HY-115913
    PDE4-IN-6
    		Inhibitor
    PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects.
    PDE4-IN-6
  • HY-15025AS
    Sildenafil citrate-d8
    Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate-d<sub>8</sub>
  • HY-19035
    DN-9693 dihydrochloride
    		Inhibitor
    DN-9693 dihydrochloride is a phosphodiesterase inhibitor with a platelet membrane effect. DN-9693 dihydrochloride can increase platelet cyclic AMP and inhibit ristocetin-induced platelet agglutination and adhesion.
    DN-9693 dihydrochloride
  • HY-N2658
    5,7-Diacetoxy-8-methoxyflavone
    		Inhibitor 98.04%
    5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase.
    5,7-Diacetoxy-8-methoxyflavone
  • HY-146889
    ATX inhibitor 16
    		Inhibitor
    ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells.
    ATX inhibitor 16
  • HY-101826A
    ER21355 hydrochloride
    		Inhibitor
    ER21355 hydrochloride is the hydrochloride form of ER21355 (HY-101826). ER21355 hydrochloride is an inhibitor for phosphodiesterase (PDE), which is potent for ameliorating benign prostatic hyperplasia (BPH) and prostatism through increasing levels of cAMP and cGMP, and resulting a relaxation of the smooth muscle cell.
    ER21355 hydrochloride
Cat. No. 상품명 / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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