A PAD inhibitor; a modified version of Cl-amidine; irreversibly inactivates all four PAD subtypes (kinact/KI = 16

BB-Cl-Amidine – 10 mg

Brand:
Cayman
CAS:
1802637-39-3
Storage:
-20
UN-No:
Non-Hazardous - /

BB-Cl-Amidine is a modified version of Cl-amidine (Item No. 10599) that retains the functional components but possesses a C-terminal benzimidazole group designed to limit proteolysis of the C-terminal amide.{27726} BB-Cl-Amidine irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} The cellular potency of BB-Cl-amidine against PAD4 is increased 20-fold over the parent compound (EC50 = 8.8 µM versus >200 µM for Cl-amidine). BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h versus ~15 min, respectively). Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.{27726} BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice.  

 

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Description

A PAD inhibitor; a modified version of Cl-amidine; irreversibly inactivates all four PAD subtypes (kinact/KI = 16,100, 4,100, 6,800, and 13,300 M-1min-1 for PAD1-4, respectively); potency is increased 20-fold over that of Cl-amidine (EC50 = 8.8 µM versus >200 µM for Cl-amidine); longer half-life than Cl-amidine (1.75 h versus ~15 min, respectively); inhibits formation of neutrophil extracellular traps

Formal name: ​N-[(1S)-1-(1H-benzimidazol-2-yl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-[1,1′-biphenyl]-4-carboxamide​​

Synonyms: 

Molecular weight: 460

CAS: 1802637-39-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deiminases||Research Area|Epigenetics, Transcription, & Translation|Writers|Citrullination||Research Area|Immunology & Inflammation|Innate Immunity|NETosis

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