[HTML][HTML] 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo
EP Garvey, JA Oplinger, ES Furfine, RJ Kiff… - Journal of Biological …, 1997 - ASBMB
N-(3-(Aminomethyl) benzyl) acetamidine (1400W) was a slow, tight binding inhibitor of
human inducible nitric-oxide synthase (iNOS). The slow onset of inhibition by 1400W
showed saturation kinetics with a maximal rate constant of 0.028 s− 1 and a binding
constant of 2.0 μM. Inhibition was dependent on the cofactor NADPH. L-Arginine was a
competitive inhibitor of 1400W binding with a K s value of 3.0 μM. Inhibited enzyme did not
recover activity after 2 h. Thus, 1400W was either an irreversible inhibitor or an extremely …
human inducible nitric-oxide synthase (iNOS). The slow onset of inhibition by 1400W
showed saturation kinetics with a maximal rate constant of 0.028 s− 1 and a binding
constant of 2.0 μM. Inhibition was dependent on the cofactor NADPH. L-Arginine was a
competitive inhibitor of 1400W binding with a K s value of 3.0 μM. Inhibited enzyme did not
recover activity after 2 h. Thus, 1400W was either an irreversible inhibitor or an extremely …