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PET-cGMP-8-TMAmd-(PEG pd 2000)-AmdMT-8-cGMP-PET

β- Phenyl- 1, N²-ethenoguanosine- 3', 5'-cyclic monophosphate- [8- thiomethylamido- (PEG pd 2000)- amidomethylthio- 8]- β- phenyl- 1, N²-ethenoguanosine- 3', 5'-cyclic monophosphate ( PET-cGMP-8-TMAmd-(PEG pd 2000)-AmdMT-8-cGMP-PET ), sodium salt

Polymer-linked dimeric (PLD) cGMP analogue
Cat. No.: P 059
    
CAS No.: [pending]
Shipping: ambient
Product Name Price (net) Qty
Cat. No.: P 059-01
Unit: 1 µmol
$353.00

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