IKK2-IN-4

IKK2-IN-4 is an orally active and selective IKK-2 inhibitor (IC₅₀ = 0.025 μM) that also inhibits JNK-1 (IC₅₀ = 1.6 μM). IKK2-IN-4 blocks IκB phosphorylation and NF-κB activation, and inhibits JNK-1 kinase activity. IKK2-IN-4 inhibits TNF-α production in PBMCs. IKK2-IN-4 can be used for research on IKK-2-related diseases, such as autoimmune diseases^[1]. In Vitro:IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor with an IKK-2 IC₅₀ of 0.025 μM; it inhibits IKK-1 with an IC₅₀ of 1.0 μM, demonstrating 40-fold selectivity^[1].
IKK2-IN-4 inhibits TNF-α production in PBMCs with a TNF cell IC₅₀ of 0.25 μM; the WST-1 toxicity IC₅₀ in PBMCs is 10 μM; Caco2 permeability is 17.7^[1].
IKK2‑IN‑4 exhibits a clearance rate of 3 μL/min/10⁶ cells in rat hepatocytes and a clearance rate of 27 μL/min/mg in human liver microsomes^[1].
IKK2-IN-4 inhibits JNK-1 with an IC₅₀ of 1.6 μM^[1].
IKK2‑IN‑4 in complex with human JNK‑1 yields an X‑ray crystal structure at 2.1 Å resolution, which validates the modelled binding mode of IKK‑2, and all predicted hydrogen bonds are observed in the X‑ray structure^[1].