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
1888 ML 130 Potent and selective inhibitor of NOD1 (NLRC1) €95.00
2641 ML334 Activator of NRF2 by inhibition of Keap1-NRF2 interactions €120.00
2671 ML385 Inhibitor of NRF2 €120.00
3046 MRT 67307 TBK1 and IKKϵ inhibitor €125.00
1258 Necrostatin-1 RIP1 inhibitor €95.00
3387 NF-κB Activation Inhibitor IV Potent NF-κB activation inhibitor €90.00
2366 NG 25 trihydrochloride Type II inhibitor of TAK1 (MAP3K7) and MAP4K2 (GCK) €75.00
3475 OLT1177 Selective and orally active NLRP3 inflammasome inhibitor €70.00
2497 Omaveloxolone Triterpenoid activator of NRF2 and inhibitor of NF-κB €90.00
2174 PD 90780 Inhibitor of NGFs binding to the P75 NGFR €95.00
2545 PF 06260933 dihydrochloride Potent and selective MAP4K4 inhibitor €85.00
3537 PFK15 Potent and specific PFKFB3 inhibitor  Recently added €80.00
2542 PFK158 Nanomolar small molecule inhibitor of PFKFB3 €90.00
1651 PHA 408 IKK-2 inhibitor €105.00
3255 Pioglitazone hydrochloride PPARγ agonist; antidiabetic drug €50.00

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