PDE4 Selective Inhibitors

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S2131	Roflumilast (B9302-107)	Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.	Selective	PDE4A1, IC50: 0.7 nM; PDE4A4, IC50: 0.9 nM; PDE4B1, IC50: 0.7 nM; PDE4B2, IC50: 0.2 nM; PDE4C1, IC50: 3 nM; PDE4C2, IC50: 4.3 nM
S0190	Lotamilast (RVT-501)	Lotamilast (RVT-501, E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.	Selective	PDE4, IC50: 2.8 nM
S0127	CP-671305	CP-671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D (PDE4-D) with IC50 of 3 nM.	Selective	PDE4-D, IC50: 3 nM
S6844	Zatolmilast (BPN14770)	Zatolmilast (BPN14770) is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.	Selective	PDE4D7, IC50: 7.8 nM; PDE4D3, IC50: 7.4 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 (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.	Selective	LPDE4, IC50: 100 nM; HPDE4, IC50: 120 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
S5014	Crisaborole (AN2728)	Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.	Selective
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.	Pan	PDE4B, IC50: 3.2 pM
S4837	Ibudilast	Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.	Pan	PDE4, IC50: 0.08 μM
S1430	Rolipram (ZK-62711)	The PDE4 selective inhibitor, Rolipram (ZK-62711, SB 95952), inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.	Pan	PDE4B, IC50: 130 nM
S2320	Luteolin	Luteolin (Luteoline, Luteolol, Digitoflavone) 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.	Pan	PDE4, Ki: 11.1 μM
S5836	IBMX	IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.	Pan	PDE4, IC50: 26.3 μM
S4090	Fenspiride HCl	Fenspiride(Decaspiride) 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