BMS 345541 (hydrochloride)

BMS 345541 is a cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50s = 4 and 0.3 µM).1 It is without effect against a panel of other serine/threonine and tyrosine kinases at 100 µM.1 BMS 345541 inhibits signaling through nuclear factor-κB (NF-κB) both in cells and in vivo, showing excellent pharmacokinetics in mice.1 It blocks joint inflammation and damage in collagen-induced arthritis in mice and induces apoptosis in melanoma cells both in vitro and in vivo.2,3 BMS 345541 is used to explore novel roles for IKK phosphorylation and NF-κB signaling.4,5WARNING This product is not for human or veterinary use.

A selective inhibitor of IKKα and IKKβ

291.8

≥98%

Biochemicals/Kinase Inhibitors/IKKs/Small Molecule Inhibitors/Kinases/TNF-α/NF-κB Signaling

Formal_Name:N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-1,2-ethanediamine, monohydrochloride;Synonyms:IKK Inhibitor III

CC1=CN=C2N1C3=C(C=CC(C)=C3)N=C2NCCN.Cl

C14H17N5 • HCl

547757-23-3

≥ 4 years

PBS (pH 7.2): 10 mg/ml

1.Burke, J.R.,Pattoli, M.A.,Gregor, K.R., et al. 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. The Journal of Biological Chemisty 278(3), 1450-1456 (2003).
2.McIntyre, K.W.,Shuster, D.J.,Gillooly, K.M., et al. A highly selective inhibitor of IκB kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice. Arthritis and Rheumatism 48(9), 2652-2659 (2003).
3.Yang, J.,Amiri, K.I.,Burke, J.R., et al. BMS-345541 targets inhibitor of κB kinase and induces apoptosis in melanoma: Involvement of nuclear factor κB and mitochondria pathways. Clinical Cancer Research 12(3 Pt 1), 950-960 (2006).
4.Karim, Z.A.,Zhang, J.,Bangerjee, M., et al. IκB kinase phosphorylation of SNAP-23 controls platelet secretion. Blood 121(22), 4567-4574 (2013).
5.Wen, L.,Zhu, M.,Madigan, M.C., et al. Immunomodulatory effects of bone marrow-derived mesenchymal stem cells on pro-inflammatory cytokine-stimulated human corneal epithelial cells. PLoS One 9(7), 1-12 (2014).