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
3350 BX 795 hydrochloride PDPK1, TBK1 and IKK inhibitor €80.00
2575 C-DIM12 Nurr1 activator that stimulates apoptosis in bladder cancer cells €85.00
2025 CC-401 ATP-competitive JNK inhibitor €115.00
2634 CC-930 Potent, selective, and orally active anti-fibrotic JNK inhibitor €95.00
1772 CDDO-Me IKK-2 inhibitor; Inducer of the Nrf2 pathway €80.00
2656 CRT0066854 Selective ATP-competitive inhibitor of the atypical PKC isoenzymes €135.00
2455 CU-T12-9 Selective TLR1/TLR2 agonist that facilitates the TLR1/2 complex formation €120.00
3216 DCZ0415 AAA-ATPase TRIP13 inhibitor  Recently added €85.00
2496 Dimethylcelecoxib, 2,5- Celecoxib analog with anti-tumor properties, lacking COX-2 inhibitory activity €75.00
2887 DRI-C21045 Inhibitor of the CD40-CD40L costimulatory protein-protein interaction €125.00
2568 EML 425 Potent reversible dual inhibitor of CBP and p300 (HAT/KAT3) €95.00
2800 Ensemble Compound 159 Cytokine inhibitor; IL-17A inhibitor Inquire
1682 Enzastaurin PKC-β inhibitor €95.00
2080 EVP 4593 NF-κB activation inhibitor; inhibits SOC pathway €110.00
2318 FC 99 hydrochloride Inhibitor of TLR3 expression and inflammatory responses. €95.00

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