IKKbeta-IN-5 is an orally active and selective IKKbeta inhibitor with an IC50 of 7.5 nM. IKKbeta-IN-5 directly inhibits IKKbeta phosphorylation and attenuates NF kappaB mediated inflammatory and survival signals while promoting autophagy flux. IKKbeta-IN-5 exhibits a 6-fold selectivity forIKKbeta over the homologous kinase IKKalpha. IKKbeta-IN-5 exerts robust antiproliferative effects through a dual mechanism involving G2/M phase cell cycle arrest and autophagy activation, even under inflammatory stimulation in vitro. IKKbeta-IN-5 demonstrates favorable pharmacokinetics and suppresses tumor growth in vivo. IKKbeta-IN-5 can be used for colorectal cancer and potentially other inflammation driven malignancies research[1].
Molekulargewicht:
417.48
Formel:
C23H24FN7
Target-Kategorie:
Autophagy,IKK,NF-kappaB
Anwendungsbeschreibung:
MCE Product type: Reference compound
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