Synonyms: ((3S,4R)-3-Amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride; AOB6992; GSK 484; GSK-484 hydrochloride; GTPL8577
Molecular Formula: C27H31N5O3 · HCl
Molecular Weight: 510.03
Linear Structural Formula: C27H31N5O3 · HCl
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC50 values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1-11 even at 100 muM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a beta-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
Other Notes: GSK484 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK484 probe summary on the Chemical Probes Portal website.