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-15747A
    Deltarasin hydrochloride
    		Inhibitor 98.07%
    Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.
    Deltarasin hydrochloride
  • 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.
    Tofisopam
  • HY-B0523
    Anagrelide
    		Inhibitor 99.87%
    Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action.
    Anagrelide
  • HY-105092
    Tetomilast
    		Inhibitor ≥98.0%
    Tetomilast (OPC-6535) is a PDE4 inhibitor with potential for the research of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD).
    Tetomilast
  • HY-B0312S
    Dipyridamole-d20
    		Inhibitor ≥98.0%
    Dipyridamole-d20 is the deuterium labeled Dipyridamole. Dipyridamole is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells[1][2][3].
    Dipyridamole-d<sub>20</sub>
  • HY-131973
    PDE10A-IN-2 hydrochloride
    		Inhibitor 98.43%
    PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
    PDE10A-IN-2 hydrochloride
  • HY-117318
    PDE12-IN-1
    		Inhibitor 98.85%
    PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.
    PDE12-IN-1
  • HY-122641
    Deltasonamide 1
    		Inhibitor 99.15%
    Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors.
    Deltasonamide 1
  • HY-122641A
    Deltasonamide 2
    		Inhibitor
    Deltasonamide 2 is a competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
    Deltasonamide 2
  • HY-U00427
    PDE2/PDE10-IN-1
    		Inhibitor 99.88%
    PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
    PDE2/PDE10-IN-1
  • HY-U00344A
    Theodrenaline hydrochloride
    		Inhibitor
    Theodrenaline hydrochloride is a cardiac stimulant, also acts as an anti-hypotensive agent together with Cafedrine.
    Theodrenaline hydrochloride
  • HY-100164
    SDZ-MKS 492
    		Inhibitor 99.77%
    SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
    SDZ-MKS 492
  • HY-117977
    FCPR03
    		Inhibitor 99.82%
    FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects.
    FCPR03
  • HY-U00344
    Theodrenaline
    		Inhibitor
    Theodrenaline is a cardiac stimulant, also acts as an anti-hypotensive agent together with cafedrine.
    Theodrenaline
  • HY-103035
    BIO-32546
    		Modulator 99.05%
    BIO-32546 (example 12b, S-isomer) is an autotaxin (ATX) modulator (IC50: 1 nM), extracted from the patent US20170158687A1.
    BIO-32546
  • HY-122641B
    Deltasonamide 2 (TFA)
    		Inhibitor 99.67%
    Deltasonamide 2 TFA is competitive, high affinity PDEδ inhibitor with a Kd of ~385 pM.
    Deltasonamide 2 (TFA)
  • HY-161853
    TX-2552
    		Inhibitor 99.69%
    TX-2552 is an orally active tyrosine DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 value of 0.62 μM. TX-2552 can enhance the clastogenic activity of Topotecan (HY-13768) in mouse bone marrow cells, as well as the anti-tumor effect of Topotecan (HY-13768) in Krebs-2 ascites tumor mice.
    TX-2552
  • HY-12788A
    (S)-PF-04449613
    		Inhibitor 99.85%
    (S)-PF-04449613 is the left-handed isomer of PF-04449613 (HY-12788). PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM. PF-04449613 improves motor learning ability in a mouse model.
    (S)-PF-04449613
  • HY-14254
    Olprinone Hydrochloride
    		Inhibitor 99.85%
    Olprinone (Loprinone) Hydrochloride is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone Hydrochloride is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
    Olprinone Hydrochloride
  • HY-143469
    NPP1-IN-1
    		Inhibitor
    NPP1-IN-1 is a potent NPP inhibitor with IC50s of 0.15 μM and 40 μM for NPP1 and NPP3, respectively.
    NPP1-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Phosphodiesterase (PDE) Isoform Comparison

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