PET-cGMP-8-TMAmd-(EO)₈-EAmdMT-8-cGMP-PET

Polymer-linked dimeric (PLD) cGMP analogue in which two cGMP units are linked by a spacer with 8 ethylene oxide units via thioethers at the C8 positions. In addition, β-phenyl-1,N2-etheno (PET) groups have been attached to both guanine nucleobases.
Membrane-permeant cGMP dimer with enhanced PKG activation properties by addressing two binding sites simultaneously with a single molecule. Activation constants of PET-cGMP-8-TMAmd-(EO)₈-EAmdMT-8-cGMP-PET in vitro on purified cGMP-dependent protein kinase (PKG) isozymes were measured to be in the range of < 1 nM (PKG1α and PKG1β) and ~35 nM (PKG2), respectively (BIOLOG in-house data).