[HTML][HTML] BMS-345541 is a highly selective inhibitor of IκB kinase that binds at an allosteric site of the enzyme and blocks NF-κB-dependent transcription in mice
JR Burke, MA Pattoli, KR Gregor, PJ Brassil… - Journal of Biological …, 2003 - ASBMB
The signal-inducible phosphorylation of serines 32 and 36 of IκBα is critical in regulating the
subsequent ubiquitination and proteolysis of IκBα, which then releases NF-κB to promote
gene transcription. The multisubunit IκB kinase responsible for this phosphorylation contains
two catalytic subunits, termed IκB kinase (IKK)-1 and IKK-2. BMS-345541 (4 (2′-
aminoethyl) amino-1, 8-dimethylimidazo (1, 2-a) quinoxaline) was identified as a selective
inhibitor of the catalytic subunits of IKK (IKK-2 IC 50= 0.3 μm, IKK-1 IC 50= 4 μm). The …
subsequent ubiquitination and proteolysis of IκBα, which then releases NF-κB to promote
gene transcription. The multisubunit IκB kinase responsible for this phosphorylation contains
two catalytic subunits, termed IκB kinase (IKK)-1 and IKK-2. BMS-345541 (4 (2′-
aminoethyl) amino-1, 8-dimethylimidazo (1, 2-a) quinoxaline) was identified as a selective
inhibitor of the catalytic subunits of IKK (IKK-2 IC 50= 0.3 μm, IKK-1 IC 50= 4 μm). The …