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
2989 15-LOX-1 inhibitor i472 Inhibitor of 15-lipoxygenase-1 (15-LOX-1) €165.00
2496 2,5-Dimethylcelecoxib Celecoxib analog with anti-tumor properties, lacking COX-2 inhibitory activity €75.00
2175 3PO Inhibitor of HIF-1-induced PFKFB3, an enzyme with a key role in glycolysis. €65.00
3631 ABR-238901 Potent S100A8/A9 blocker €170.00
2552 Adjudin Non-hormonal male contraceptive with anti-proliferative activity €125.00
1291 AEG 3482 JNK inhibitor €85.00
2500 Apilimod dimesylate Cytokine inhibitor; IL-12 and IL-23 inhibitor €110.00
2611 APS-2-79 Inhibitor of KSR and oncogenic Ras signaling €90.00
2819 APX-115 First-in-class pan-NADPH oxidase (Nox) inhibitor €125.00
2307 ARM1 hydrobromide Novel type of LTA4H inhibitor that selectively blocks the conversion of LTA4 into LTB4 €92.00
5051 Axon Ligands™ Cell signaling and Oncology compound library Axon Ligands™ Cell signaling and Oncology compound library Inquire
2132 BAY 11-7082 IKK inhibitor and anti-inflammatory €85.00
2178 BCI Allosteric inhibitor of dual-specificity phosphatases (DUSP) €75.00
2852 BCI hydrochloride Allosteric inhibitor of dual-specificity phosphatases (DUSP) €75.00
2002 Bentamapimod JNK inhibitor, which inhibited JNK1, JNK2 and JNK3 €70.00
1731 BMS 345541 Cell-permeable and selective IKB (IKK) inhibitor €105.00
3664 Brivudine Inhibitor of herpes virus DNA polymerase €90.00
3437 BTYNB Potent and selective IMP1 inhibitor €90.00
1390 BX 795 PDPK1, TBK1 and IKK inhibitor €60.00
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 €85.00
3518 DCZ0805 NF-κB activation inhibitor €130.00
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

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