For other salt forms please inquire. Polymer-linked dimeric (PLD) cGMP analogue in which two cGMP units are linked by a polydisperse 2000 Dalton spacer on basis of polyethylene glycol (PEG) via thio-functions 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-(PEG pd 2000)-AmdMT-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 ~80 nM (PKG2), respectively (BIOLOG in-house data).
PET-cGMP-8-TMAmd-(PEG pd 2000)-AmdMT-8-cGMP-PET decreased cell viability in the PKG2 expressing colon cancer cell line Caco-2, but not in the PKG2 expressing colon cancer cell lines HCT 116 and HT-29. Reference: Hoffmann et al., Eur. J. Med. Chem., 141, 61-72 (2017).
| Cat. No. | P 059 |
| CAS number | [pending] |
| Purity | > 95% HPLC (est.) |
| Salt form | Disodium |
| Storage temperature | -20°C / -4°F |
| Modifications | 1-cGMP, 2-cGMP, 8-cGMP |
| Target | PKG (cGK) Activator |
| Absorption max [nm] | 272 |
| Molar extinction coefficient ε [L·mol⁻¹·cm⁻¹] | 72000 |
| UV pH value | 7 |
