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
2132 BAY 11-7082 IKK inhibitor and anti-inflammatory €85.00
1731 BMS 345541 Cell-permeable and selective IKB (IKK) inhibitor €105.00
1390 BX 795 PDPK1, TBK1 and IKK inhibitor €60.00
3350 BX 795 hydrochloride PDPK1, TBK1 and IKK inhibitor €80.00
1772 CDDO-Me IKK-2 inhibitor; Inducer of the Nrf2 pathway €80.00
2725 IMD-0354 IKK-2 inhibitor €90.00
3484 IMD-0560 Selective IKK-2 inhibitor €120.00
3046 MRT 67307 TBK1 and IKKϵ inhibitor €125.00
1651 PHA 408 IKK-2 inhibitor €110.00
1568 PS 1145 IKK inhibitor €90.00
3536 SC-514 Potent, selective, reversible and ATP-competitive IKK-2 inhibitor €60.00
2070 Sulfasalazine IKK inhibitor €45.00
3889 Vinpocetine Brain-penetrant PDE/IKK inhibitor; Na+ channel blocker €50.00

13 Item(s)

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