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-145319
    FPFT-2216
    		Inhibitor 99.35%
    FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.
    FPFT-2216
  • HY-109586
    BRL-50481
    		Inhibitor 99.85%
    BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
    BRL-50481
  • HY-14286
    Levosimendan
    		Inhibitor 99.88%
    Levosimendan (Simsndan; OR-1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.
    Levosimendan
  • HY-128358
    MR-L2
    		Activator 99.23%
    MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
    MR-L2
  • HY-50098
    Mardepodect
    		Inhibitor 99.69%
    Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
    Mardepodect
  • HY-147389
    Enpp-1-IN-14
    		Inhibitor 99.87%
    Enpp-1-IN-14 (Compound 015) is a potent Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) inhibitor with an IC50 value of 32.38 nM for recombinant human ENPP-1. Enpp-1-IN-14 has anti-tumor activity.
    Enpp-1-IN-14
  • HY-12472
    Balipodect
    		Inhibitor 98.91%
    Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
    Balipodect
  • HY-18740A
    Trequinsin hydrochloride
    		Inhibitor 99.93%
    Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of platelet CAMP phosphodiesterase (PDE), with an IC50 of 0.25 nM. Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of the aggregation of human platelets induced in vitro by ADP, collagen, thrombin and epinephrine.
    Trequinsin hydrochloride
  • HY-B0442
    Vardenafil
    		Inhibitor 99.58%
    Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
    Vardenafil
  • HY-15747
    Deltarasin
    		Inhibitor 99.89%
    Deltarasin is an inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
    Deltarasin
  • HY-15485
    Zardaverine
    		Inhibitor 98.73%
    Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
    Zardaverine
  • HY-145924
    BAY 2666605
    		Inhibitor 99.64%
    BAY 2666605 is an orally active PDE3A and PDE3B inhibitor with IC50s of 87 nM and 50 nM, respectively. BAY 2666605 is a PDE3A-SLFN12 complex inducer (WO2019025562A1; example 135).
    BAY 2666605
  • HY-10469
    GSK256066
    		Inhibitor 98.15%
    GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.
    GSK256066
  • HY-109085
    Difamilast
    		Inhibitor 99.63%
    Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).
    Difamilast
  • HY-14930A
    Mirodenafil dihydrochloride
    		Inhibitor 99.85%
    Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil dihydrochloride
  • HY-19329
    HA130
    		Inhibitor 99.46%
    HA130 is a selective autotaxin (ATX) inhibitor with an IC50 of 28 nM.
    HA130
  • HY-10790
    Cilomilast
    		Inhibitor 99.89%
    Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
    Cilomilast
  • HY-124772
    BI-2545
    		Inhibitor 99.77%
    BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively.
    BI-2545
  • HY-108618
    BC11-38
    		Inhibitor 99.42%
    BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
    BC11-38
  • HY-110137
    Furamidine dihydrochloride
    		Inhibitor ≥99.0%
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
    Furamidine dihydrochloride
Phosphodiesterase (PDE) Isoform Comparison

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