GSK256066

  • Chemical Properties
CAS No. 801312-28-7 Cat. No. BCP02627
Name GSK256066
Synonyms GSK-256066;GSK 256066;
Formula C27H26N4O5S M. Wt 518.58
  • Biological Activity
Description GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity.
Pathways Protease/Metabolic Enzyme 
Targets Phosphodiesterase/PDE 

Structure

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