The IKK kinase complex is the core element of the NF-κB cascade (see section of Axon Ligands™ interacting with NF-κB signaling). It is essentially made of two kinases (IKKα (or IKK-1) and IKKβ (or IKK-2); EC and a regulatory subunit, NEMO/IKKγ. NF-κB represents a family of transcription factors that are normally kept inactive in the cytoplasm through interaction with inhibitory molecules of the IκB family. In response to multiple stimuli such as inflammatory cytokines, bacterial or viral products, or various types of stress, the IκB molecules become phosphorylated on two critical serine residues. This modification is recognized by a specific E3 ubiquitin ligase complex and undergoes polyubiquitination, which targets them for rapid degradation by the 26S proteasome[1]. As a consequence, free NF-κB enters the nucleus and activates transcription of a variety of genes participating in the immune and inflammatory response, cell adhesion, growth control, and protection against apoptosis[2].

[1] The IkB kinase IKK andNF- kB: key elements of proinflammatory signaling. M. Karin, M. Delhase. Semin. Immunol. 2000, 12, 85-98.
[2] The IKK Complex, a Central Regulator of NF-κB Activation. A. Israël. Cold Spring Harb Perspect Biol 2010, 2, a000158.

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Axon ID Name Description From price
2070 Sulfasalazine IKK inhibitor €45.00
1568 PS 1145 IKK inhibitor €95.00
1651 PHA 408 IKK-2 inhibitor €105.00
2725 IMD-0354 IKK-2 inhibitor €90.00
1772 CDDO-Me IKK-2 inhibitor; Inducer of the Nrf2 pathway €80.00
1731 BMS 345541 Cell-permeable and selective IKB (IKK) inhibitor €105.00
2132 BAY 11-7082 IKK inhibitor and anti-inflammatory €85.00

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