| 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 |
