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.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
2989 | 15-LOX-1 inhibitor i472 | Inhibitor of 15-lipoxygenase-1 (15-LOX-1) | €170.00 | |
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 | €90.00 | |
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 | |
3904 | BAY-0069 | Potent covalent PPARγ inverse agonist | €90.00 | |
3809 | BAY-4931 | Potent covalent PPARγ inverse agonist | €120.00 | |
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 | |
3877 | BMS-986299 | First-in-class NLRP3 agonist | €140.00 | |
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 | |
3846 | C25-140 | First-in-class TRAF6–Ubc13 inhibitor | €160.00 | |
3981 | Calcium influx inducer compound 634 | Ca2+ influx inducer | €130.00 | |
2025 | CC-401 | ATP-competitive JNK inhibitor | €120.00 | |
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 | |
4066 | CM-4620 | Selective Orai1 channel inhibitor; SOCE inhibitor | €150.00 |