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 | |
---|---|---|---|---|
3410 | UTL-5g | TNFα modulator | €120.00 | |
1507 | TMI 005 | TACE/MMP inhibitor | €150.00 | |
2193 | Thioridazine hydrochloride | DA and α1 adrenoceptor antagonist; MALT1 inhibitor | €50.00 | |
3324 | Thalidomide | TNFα inhibitor. Immunomodulator. | €50.00 | |
2339 | TH 1834 | Tip60 histone acetyltransferase inhibitor | €140.00 | |
3282 | Takinib | Potent and selective TAK1 (MAP3K7) inhibitor | €105.00 | |
2263 | Tacrolimus | Potent Calcineurin (Ca2+ dependent protein phosphatase 2B) inhibitor | €100.00 | |
2070 | Sulfasalazine | IKK inhibitor | €45.00 | |
2365 | SR 3576 | Very potent JNK3 inhibitor with >2800-fold selectivity over p38 | €135.00 | |
2143 | SPD 304 | Cell permeable inhibitor of TNFα | €145.00 | |
2519 | SP 600125 | Selective, reversible, and ATP-competitive JNK inhibitor | €70.00 | |
1635 | Sotrastaurin | PKC inhibitor | €50.00 | |
2487 | Silibinin | Natural flavonolignan, cytoprotectant, antioxidant, and antihepatotoxic agent | €40.00 | |
3536 | SC-514 | Potent, selective, reversible and ATP-competitive IKK-2 inhibitor | €60.00 | |
2444 | SB 706504 | Selective p38 MAPK inhibitor that targets a subset of inflammatory macrophage genes. | €125.00 | |
2666 | S-Propargyl-Cysteine | Modulator of endogenous hydrogen disulfide | €95.00 | |
2443 | Rosiglitazone | PPARγ agonist; antidiabetic drug and stem cell differentiator | €95.00 | |
2677 | RIPA-56 | RIP1 inhibitor for the treatment of systemic inflammatory response syndrome | €60.00 | |
1568 | PS 1145 | IKK inhibitor | €90.00 | |
3166 | Pomalidomide | TNFα inhibitor. Immunomodulator. | €60.00 | |
2647 | Pirfenidone | Broad-spectrum anti-inflammatory and anti-fibrosis agent | €60.00 | |
2488 | Piperlongumine | Natural alkaloid with potent cytotoxic activity | €65.00 | |
3255 | Pioglitazone hydrochloride | PPARγ agonist; antidiabetic drug | €50.00 | |
1651 | PHA 408 | IKK-2 inhibitor | €110.00 | |
2542 | PFK158 | Nanomolar small molecule inhibitor of PFKFB3 | €90.00 | |
3537 | PFK15 | Potent and specific PFKFB3 inhibitor | €80.00 | |
2545 | PF 06260933 dihydrochloride | Potent and selective MAP4K4 inhibitor | €85.00 | |
2174 | PD90780 | Inhibitor of NGFs binding to the P75 NGFR | €110.00 | |
3614 | Parthenolide | NF-κB activation inhibitor | €90.00 | |
2497 | Omaveloxolone | Triterpenoid activator of NRF2 and inhibitor of NF-κB | €90.00 |