Synonyms: GSK 484 | GSK-484
Compound class:
Synthetic organic
Comment: GSK484 binds to peptidyl arginine deiminase, type IV (PADI4; Q9UM07) and inhibits its activity [1]. PADI4 contributes to regulating the histone code by effecting the citrullination/deimination of histones. PADI4 has strong associations with cancer and immune and inflammatory processes. GSK484 will be a useful tool to enhance understanding of the normal and pathological functions of PADI4.
This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection, developed in collaboration with GlaxoSmithKline (GSK). |
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Bioactivity Comments |
GSK484 binds to PADI4 reversibly and is substrate-competitive, with an IC50 of 50 nM in the absence of calcium (250nM @ 2mM calcium) [1]. The phramacodynamic and pharmacokinetic profiles of GSK484 suggest that has potential as an in vivo tool. |