An inhibitor of IKK2
Inhibitor of NF-κB kinase 2 (IKK2, also known as IKKβ) acts as part of an IKK complex in the canonical NF-κB pathway, phosphorylating inhibitors of NF-κB (IκBs) to initiate signaling. NF-κB signaling can also occur through a non-canonical, IKK/IκB-independent pathway. IKK2 Inhibitor VI is a potent, cell-permeable, reversible inhibitor of IKK2 (IC50 = 13 nM). [1] It is used to evaluate the role of the canonical, IκB-dependent NF-κB signaling pathway in cellular responses.[2][3]
Reference:
[1]. Baxter, A., Brough, S., Cooper, A., et al. Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorganic & Medicinal Chemistry Letters 14, 2817-2822 (2004).
[2]. McNamara, L.A., Ganesh, J.A., and Collins, K.L. Latent HIV-1 infection occurs in multiple subsets of hematopoietic progenitor cells and is reversed by NF-κB activation. Journal of Virology 86(17), 9337-9350 (2012).
[3]. Punj, V., Matta, H., and Chaudhary, P.M. A computational profiling of changes in gene expression and transcription factors induced by vFLIP K13 in primary effusion lymphoma. PLoS One 7(5), 1-15 (2012).
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