Propenyl-L-NIO . hydrochloride

Potent, selective inhibitor of iNOS (NOS II). The K_i values for inhibition of iNOS (NOS II), nNOS (NOS I), and eNOS (NOS III) by ENIPO are 17, 10.3 and 58.2 µM, respectively, as determined using initial rate binding kinetics. However, ENIPO is a time-dependent inhibitor that, with longer incubations, demonstrates reversible tight binding inhibition that is selective for iNOS (NOS II) over nNOS (NOS I) or eNOS (NOS III). This selectivity results from iNOS (NOS II) exhibiting a 4-fold faster binding and 10-fold slower dissociation with ENIPO compared to nNOS (NOS I). K_i values for ENIPO binding to iNOS (NOS II) and nNOS (NOS I) are 0.56 and 6 µM, respectively. Accurate determination of the K_i value of ENIPO for eNOS (NOS III) has not been determined but is expected to be 50-fold less than iNOS (NOS II).