BI605906, also called SCHEMBL4470165, is a novel pharmacological inhibitor of TNFα-dependent IκB degradation. In additonally, it also inhits expression of pro-inflammatory mediators IL-6, IL-1b, and CXCL1/2. IKKβ: IC50= 380 nM (when assayed at 0.1 mM ATP) In vitro: BI605906 not only prevents the phosphorylation of physiological substrates, such as p105 and RelA, but also the phosphorylation of the serine residues in IKKβ (Ser177 and Ser181) that trigger its activation.
Wow, nice. I wonder what the next breakthrough will be.
I have no idea what this means…
Neither do I, but it sounds exciting (lol) ^^.