GSK256066 is a selective PDE4 inhibitor with an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 vs. other PDE isoforms. Often used clinically by inhalation in chronic obstructive pulmonary disease and asthma.

6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide

IC50 =3.2 pM for PDE4B, with >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. GSK256066 inhibits PDE4 isoforms A-D with equal affinity.

Soluble in DMSO (>4.6 mg/mL). Minimal solubility in water (< 1.2 mg/mL)

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

1. Tralau-Stewart CJ, et al. J Pharmacol Exp Ther, 2011, 337(1), 145-154.
2. Woodrow MD, et al. Bioorg Med Chem Lett, 2009, 19(17), 5261-5265.

PDE Inhibitor

Inhibitor