0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP[1].
0990CL (100 nM-1 μM; 24 hours) is able to restore α2AR/Gαi mediated cAMP levels elicited by Fsk and UK14304 in HEK293 GloSensor cells. When the dosage is at 100 nM, it restores 31% of the reduction of cAMP[1].
0990CL (30 μM; pre-treatment 30mins) shows selectivity for Gαi1 over Gαq. It demonstrates selectivity for Gαi and Gαq and results in a maximum endpoint fluorescence reduction of 38±8% and 10%, respectively[1].