Photoswitchable PAD Inhibitor (technical grade)

A photoactivated PAD inhibitor

Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine (Item No. 17079) that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 µM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2 when used at concentrations up to 100 µM. However, it 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.

488

≥70% (mixture of isomers)

O=C(N[C@@H](CCCNC(CCl)=N)C1=NC2=C(C=CC=C2)N1)C(C=C3)=CC=C3/N=N/C4=CC=CC=C4

C26H26ClN7O

2226393-62-8

≥ 2 years

Methanol: 30 mg/ml