Cayman Chemical PhotoswItchable PAD InhIbItr
A photoactivated PAD inhibitor; a weak inhibitor of PAD2 (IC50 = >100 µM) and less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 for M-1min-1 for PAD1-4, respectively) without photoactivation; can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 µM