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BMS-345541(free base) is a selective inhibitor of IKK-1 and IKK-2 with IC50 value of 4μM and 0.3μM, respectively [1].

IKK is also known as nuclear factor kappa-B kinase subunit inhibitor and involves in cytokine-activated intracellular signaling pathways. IKK-1 and IKK-2 are members of IKK family. It has been reported that IKK-2 plays a pivotal role in brain cells following a stroke [2] [3].

BMS-345541 is a potent IKK inhibitor and has a highly selective activity compared with other kinases. When tested with THP-1 monocytic cells, pre-incubation with BMS-345541 inhibited TNF-α-stimulated IKK phosphorylation and reduced a variety of cytokines production including TNF-α, IL-1β, IL-8, and IL-6 [1]. In 4 human glioma cell lines, BMS-345541 treatment significantly blocked cell proliferation (80%-95%) at the concentration of 10 μM or higher and also inhibited IL-8 expression in a dose dependent manner (IC50>2 μM) [2]. And similar result of BMS-34551 inhibition on IKK which induced cell apoptosis was verified in human melanoma cell lines SK-MEL-5, Hs 294T, and A375 [3].

In 18-22g female BALB/c mice model, administration of BMS-345541 inhibited TNF-αproduction in a dose-dependent manner, ~50% inhibition was seen when used the concentration of 10 mg/kg and near complete inhibition was seen at a dose of 100 mg/kg [1].

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