ic-87201

Description: IC87201 is an inhibitor of PSD95-nNOS protein-protein interactions. It suppresses NMDAR-dependent NO and cGMP formation. In vitro, IC87201 does not interact with the PDZ domains of nNOS or PSD-95, nor inhibit the nNOS-PDZ/PSD-95-PDZ interface by interacting with the beta-finger of nNOS-PDZ. IC87201 binds to the beta-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 also shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe. IC87201 (10 and 100 nM) attenuats NMDA/glycine-induced decreases in neurite outgrowth. IC87201 dose-dependently reduces NMDA-induced cGMP production in primary hippocampal neurons (DIV 14-21) with an IC50 of 2.7 uM. IC87201 increases the number of branches at 10-30 uM when compared to control-treated neurons.

References: Sci Rep. 2015 Jul 16; 5:12157; Neuroscience. 2015 Aug 20; 301:421-38; Behav Brain Res. 2016 May 15; 305:23-9.