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Apexbio Technology LLC I-BET-762 1260907-17-2 10mM (in 1mL DMSO)
Supplier: Apexbio Technology LLC B14985.1
I-BET-762 (CAS 1260907-17-2) is a small-molecule inhibitor targeting the BET (bromodomain and extra-terminal) family of proteins It acts by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains thereby displacing acetylated histones with an IC50 ranging from 32 5 to 42 5 nM and a dissociation constant (Kd) between 50 5 and 61 3 nM I-BET-762 displays high selectivity exhibiting no interaction with non-BET bromodomain-containing proteins In cellular studies it downregulates LPS-induced gene expression resulting in reduced production of pro-inflammatory cytokines and chemokines In vivo models demonstrate its potential to attenuate features of established inflammatory disease supporting its utility in epigenetic and inflammation-related research
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