Description | GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium. | ||
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Targets |
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In vitro | GSK484 also inhibits PAD4 citrullination (at 0.2 mM calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay. GSK484 causes a clear, statistically-significant reduction in diffused NETs.[1] | ||
In vivo | GSK484 prevents tumor-induced NETosis in vivo and can antagonize kidney injury in mice with mammary carcinoma or pancreatic neuroendocrine tumors.[2] |