Description
BMS-345541 is a highly selective inhibitor of IKK-1 and IKK-2 with IC50 values of 4 μM and 0.3 μM, respectively.
Product Overview
BMS-345541 is a highly selective inhibitor of IKK-1 and IKK-2 with IC50 values of 4μM and 0.3μM, respectively. BMS-345541 is a highly selective inhibitor of IKK that inhibits NF-κB-dependent transcription of pro-inflammatory cytokines both in vitro and in vivo. This specificity is proved in the assay measuring the IKK-2-catalyzed phosphorylation of GST-IκB. In this assay, BMS-345541 fails to inhibit other serine/threonine and tyrosine kinases. This selectivity is also evident in cells, only the stimulus-induced phosphorylation of IκB was inhibited by BMS-345541 whereas other signal transduction cascades were unaffected. Since the IKK/ NFκB pathway is important for viability of leukemic cells and is a predictor of relapse in T-ALL, BMS-345541 is tested in some T-ALL cell lines. It is found that BMS-345541 can induce apoptosis and an accumulation of cells in the G2/M phase of the cell cycle. BMS-345541 can be used in combination with traditional therapies to overcome resistance to chemotherapeutic agents
Synonyms
BMS-345541 hydrochloride; BMS 345541 hydrochloride
Molecular Formula
C14H18ClN5
Chemical Name
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine; hydrochloride
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request