PDE4 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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.

Selective PDE4B, IC50: 3.2 pM
S2131 Roflumilast

Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.

Selective PDE4C2, IC50: 4.3 nM; PDE4C1, IC50: 3 nM; PDE4B2, IC50: 0.2 nM; PDE4B1, IC50: 0.7 nM; PDE4A4, IC50: 0.9 nM; PDE4A1, IC50: 0.7 nM
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.

Selective PDE4, IC50: 74 nM
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.

Selective HPDE4, IC50: 120 nM; LPDE4, IC50: 100 nM
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.

Selective PDE4, IC50: 0.75 μM
S1430 Rolipram

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

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.

Pan PDE4, Ki: 11.1 μM
S4090 Fenspiride HCl

Fenspiride is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.

Pan PDE4, pIC50: 4.16