1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)

Phosphodiesterase (PDE)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-142644
    ATX inhibitor 7
    Inhibitor
    ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure.
    ATX inhibitor 7
  • HY-W011293R
    DTA (Standard)
    Inhibitor
    DTA (Standard) is the analytical standard of DTA. This product is intended for research and analytical applications. DTA (2,4-Disulfamyl-5-trifluoromethylaniline) is a cyclic AMP phosphodiesterase inhibitor that binds to erythrocyte carbonic anhydrase.
    DTA (Standard)
  • HY-W705784
    T-1032 free base
    Inhibitor
    T-1032 free base is a selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 value of 1.0 nM. T-1032 free base shows relaxant effect on isolated rabbit corpus cavernosum. T-1032 free base can be used for the research of erectile dysfunction.
    T-1032 free base
  • HY-176874
    Enpp-1-IN-29
    Inhibitor
    Enpp-1-IN-29 (Compound 1) is a highly selective ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor (IC50=0.05 nM). Enpp-1-IN-29 is promising for research of ENPP1-overexpressing cancers (e.g., breast cancer, head/neck cancer, metastatic chromosome-unstable tumors) and immune-related diseases (e.g., autoimmune disorders, tumor immune evasion).
    Enpp-1-IN-29
  • HY-106325
    AA 2379
    Inhibitor
    AA 2379 is an orally active antirheumatic agent. AA 2379 has antiinflammatory, antipyretic activities and reduces pain sensation.
    AA 2379
  • HY-131710
    PDE5-IN-3
    Inhibitor
    PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
    PDE5-IN-3
  • HY-106045A
    Imazodan hydrochloride
    Inhibitor
    Imazodan hydrochloride is the hydrochloride form of Imazodan (HY-106045). Imazodan hydrochloride is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan hydrochloride serves also as a peripheral vasodilator.
    Imazodan hydrochloride
  • HY-N3464
    Isopedicin
    Inhibitor
    Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity.
    Isopedicin
  • HY-168147
    Enpp-1-IN-24
    Inhibitor
    Enpp-1-IN-24 (compund 7) is an ENPP1 inhibitor that, in combination with anti-PD-1 antibodies, achieves 77.7% tumor growth inhibition and improves survival in mouse models.
    Enpp-1-IN-24
  • HY-117605S
    N-Desmethyl Sildenafil-d8
    99.3%
    N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
    N-Desmethyl Sildenafil-d<sub>8</sub>
  • HY-170435
    PDE5-IN-13
    Inhibitor
    PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.
    PDE5-IN-13
  • HY-174405
    PROTAC PDE4 degrader-1
    Degrader
    PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model. Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC PDE4 degrader-1
  • HY-157457
    Z21090
    Inhibitor
    Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research.
    Z21090
  • HY-123446
    JNJ-42259152
    JNJ-42259152 is a phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer that is specific for PDE10A activity. JNJ-42259152 can be dynamically scanned in healthy volunteers to assess its kinetic properties in the brain. The half-life of JNJ-42259152 in the blood is an average of 90 minutes. JNJ-42259152 has demonstrated reliable binding potential (BPND) in different target areas (such as the lentiform nucleus, caudate nucleus, ventral striatum, etc.), providing an important tool for studying neuropsychiatric diseases.
    JNJ-42259152
  • HY-160991
    Menabitan
    Inhibitor
    Menabitan (SP-204) is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan lowers the intraocular pressure in rabbit model.
    Menabitan
  • HY-107022
    BMS-341400
    Inhibitor
    BMS-341400 is an orally active selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 value of 0.3 nM. BMS-341400 reduces the degradation of cyclic guanosine monophosphate (cGMP), thereby enhancing nitric oxide (NO)-mediated relaxation of the smooth muscle of the corpus cavernosum and promoting erection. BMS-341400 can be used to study erectile dysfunction.
    BMS-341400
  • HY-115269
    CK-2289
    Inhibitor
    CK-2289 is an inhibitor of type III cyclic 3'5'-adenosine monophosphate phosphodiesterase (PDE). CK-2289 can inhibit platelet aggregation and decreases mean arterial blood pressure. CK-2289 can be used for the research of cardiovascular disease, such as congestive heart failure.
    CK-2289
  • HY-B0442BR
    Vardenafil hydrochloride trihydrate (Standard)
    Inhibitor
    Vardenafil (hydrochloride trihydrate) (Standard) is the analytical standard of Vardenafil (hydrochloride trihydrate). This product is intended for research and analytical applications. Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes-.
    Vardenafil hydrochloride trihydrate (Standard)
  • HY-169258
    PDE4-IN-21
    Inhibitor
    PDE4-IN-21 (Compound L19) is a poetent PDE4 inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitory activity and remarkable metabolic stability in rat liver microsomes.
    PDE4-IN-21
  • HY-175689
    PDEδ-IN-1
    Inhibitor
    PDEδ-IN-1 is the ligand of PDEδ. PDEδ-IN-1 can be used to synthesize PDEδ autophagic degrader 1 (HY-157458).
    PDEδ-IN-1
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