NF-κB

The NF-κB signaling pathway is involved in a broad range of biological processes including innate and adaptive immunity, inflammation, stress responses, B-cell development, and lymphoid organogenesis. A remarkable diversity of stimuli lead to the activation of NF-κB, among which are pro-inflammatory cytokines, LPS, growth factors, and antigen receptors. They activate an IKK complex (IKKβ, IKKα, and NEMO), which phosphorylates IκB proteins. Phosphorylation of IκB leads to its ubiquitination and proteasomal degradation, freeing NF-κB/Rel complexes. Active NF-κB/Rel complexes are further activated by phosphorylation and translocate to the nucleus where, either alone or in combination with other transcription factor families including AP-1, Ets, and Stat, they induce target gene expression[1],[2]. The core elements of NF-κB signaling pathways are generally several steps removed from the receptor itself. The intervening steps between receptor and IKK form links to parallel signaling pathways. For example, PKC enzymes play important roles in several signal transduction cascades. In NF-κB signaling, PKC-β connects the B cell receptor to canonical activation of NF-κB through a signaling complex, including Bcl10/MALT1 and NEMO/IKKγ[3].


[1] M.S. Hayden, S. Ghosh. Shared principles in NF-kappaB signaling. Cell. 2008, 132, 344-362.
[2]  Rel/NF-κB Transcription Factors. Gilmore TD. http://www.bu.edu/nf-kb/ 2008.
[3] Protein Kinase C-β-Dependent Activation of NF-κB in Stromal Cells Is Indispensable for the Survival of Chronic Lymphocytic Leukemia B Cells In Vivo. G. Lutzny et al. Cancer Cell. 2013, 23, 77-92.

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Axon ID Name Description From price
5051 Axon Ligands™ Cell signaling and Oncology compound library Axon Ligands™ Cell signaling and Oncology compound library Inquire
2656 CRT0066854 Selective ATP-competitive inhibitor of the atypical PKC isoenzymes €135.00
1682 Enzastaurin PKC-β inhibitor €95.00
2466 Gö 6983 Broad spectrum PKC inhibitor lacking inhibitory effect for PKCμ €90.00
2713 GSK 2982772 Specific inhibitor of RIP1 kinase €115.00
2608 GSK481 Potent inhibitor of RIP1 kinase and TNF induced inflammation €95.00
2362 LY 333531 hydrochloride PKC-β inhibitor €75.00
1401 LY 333531 mesylate PKC-β inhibitor €75.00
1258 Necrostatin-1 RIP1 inhibitor €95.00
2677 RIPA-56 RIP1 inhibitor for the treatment of systemic inflammatory response syndrome €60.00
1635 Sotrastaurin PKC inhibitor €75.00

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