PDE

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S2131

Roflumilast

Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

S1431

Sildenafil Citrate

Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

S1455

Cilomilast

Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

S1512

Tadalafil

Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay.

S2515

Vardenafil HCl Trihydrate

Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

S8459New

TAK-063

TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.

S4684New

Sildenafil

Sildenafil is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

S4683New

Sildenafil Mesylate

Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

S1550

Pimobendan

Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

S2620

GSK256066

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.

S2687

PF-2545920

PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

S1430

Rolipram

Rolipram is a PDE4 inhibitor and an anti-inflammatory agent.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1294

Cilostazol

Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

S2484

Milrinone

Milrinone is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.

S4019

Avanafil

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

S2127

S- (+)-Rolipram

S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.

S1673

Aminophylline

Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.

S3172

Anagrelide HCl

Anagrelide is a drug used for the treatment of essential thrombocytosis.

S1504

Dyphylline

Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.

S1895

Dipyridamole

Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.

S4164

Doxofylline

Doxofylline is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

S2312

Icariin

Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.

S2320

Luteolin

Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S2131

Roflumilast

Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

S1431

Sildenafil Citrate

Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.

S1455

Cilomilast

Cilomilast is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

S1512

Tadalafil

Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay.

S2515

Vardenafil HCl Trihydrate

Vardenafil HCl Trihydrate is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

S8459New

TAK-063

TAK-063 is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.

S4684New

Sildenafil

Sildenafil is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.

S4683New

Sildenafil Mesylate

Sildenafil Mesylate is a mesylate form of Sildenafil, an inhibitor of Phosphodiesterase 5.

S1550

Pimobendan

Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

S2620

GSK256066

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.

S2687

PF-2545920

PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

S1430

Rolipram

Rolipram is a PDE4 inhibitor and an anti-inflammatory agent.

S8034

Apremilast (CC-10004)

Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.

S1294

Cilostazol

Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

S2484

Milrinone

Milrinone is a phosphodiesterase 3 (PDE3) inhibitor, used to increase the heart's contractility.

S4019

Avanafil

Avanafil is a highly selective PDE5 inhibitor with IC50 of 5.2 nM, >121-fold selectivity over other PDEs.

S2127

S- (+)-Rolipram

S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.

S1673

Aminophylline

Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a nonselective adenosine receptor antagonist.

S3172

Anagrelide HCl

Anagrelide is a drug used for the treatment of essential thrombocytosis.

S1504

Dyphylline

Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects.

S1895

Dipyridamole

Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells.

S4164

Doxofylline

Doxofylline is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

S2312

Icariin

Icariin is a cGMP-specific PDE5 inhibitor with IC50 of 0.432 μM, 167-fold more selective for PDE5 than PDE4.

S2320

Luteolin

Luteolin is a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. Phase 2.