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

Photoswitchable PAD Inhibitor (technical grade) – 1 mg

Brand:
Cayman
CAS:
2226393-62-8
Storage:
-20
UN-No:
Non-Hazardous - /

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.{35916} 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.  

 

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SKU: 28104 - 1 mg Category:

Description

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

Formal name: N-[(1S)-1-(1H-benzimidazol-2-yl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-4-(2-phenyldiazenyl)-benzamide

Synonyms: 

Molecular weight: 488

CAS: 2226393-62-8

Purity: ≥70% (mixture of isomers)

Formulation: A crystalline solid

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