BMS-345541 hydrochloride is an anti-inflammatory, cell-permeable quinoxaline compound with a highly selective IKKbeta inhibitory activity. BMS-345541 blocks both joint inflammation and destruction in collagen-induced arthritis in mice. BMS-345541 hydrochloride induced apoptosis and an accumulation of cells in the G 2/M phase of the cell cycle via inhibition of IKK/NFκB signaling. T-ALL cells treated with BMS-345541 displayed nuclear translocation of FOXO3a and restoration of its functions, including control of p21(Cip1) expression levels. BMS-345541 hydrochloride is an allosteric site-binding inhibitor with a primary target of IKK-2 and blocks the NF-κB-dependent transcription in mice.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Activity of the selective IκB kinase inhibitor BMS-345541 against T-cell acute lymphoblastic leukemia: involvement of FOXO3a.
Buontempo F, et al. Cell Cycle. 2012 Jul 1;11(13):2467-75. PMID: 22713244.
BMS-345541 targets inhibitor of kappaB kinase and induces apoptosis in melanoma: involvement of nuclear factor kappaB and mitochondria pathways.
Yang J, et al. Clin Cancer Res. 2006 Feb 1;12(3 Pt 1):950-60. PMID: 16467110.
A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice.
McIntyre KW, et al. Arthritis Rheum. 2003 Sep;48(9):2652-9. PMID: 13130486.
BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.
Burke JR, et al. J Biol Chem. 2003 Jan 17;278(3):1450-6. PMID: 12403772.
|Related IκB/IKK Products|
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Bardoxolone is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.
Amlexanox is a specific inhibitor of IKKε and TBK1.
PHA-408 is a highly selective and ATP-competitive IKK-2 inhibitor with IC50 of 40 nM.
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