Helenalin acetate, a natural NF-κB inhibitor, is a potent C/EBPβ inhibitor. Helenalin acetate has anti-inflammatory and anticancer activities.
Helenalin acetate (0.1-1 μM; for 7 days) inhibits the differentiation significantly in 3T3-L1 cells[1].Helenalin acetate exerts anti-proliferative effects in acute myeloid leukemia cells but not in normal hematopoietic progenitor cells[1]. Helenalin acetate inhibits C/EBPβ by binding to the N-terminal part of C/EBPβ, thereby disrupting the cooperation of C/EBPβ with the co-activator p300. Helenalin acetate selectively inhibits only the full-length (liver-enriched activating protein* (LAP*)) isoform but not the slightly shorter (LAP) isoform[1].
References:
[1]. Jakobs A, et al. Helenalin Acetate, a Natural Sesquiterpene Lactone with Anti-inflammatory and Anti-cancer Activity, Disrupts the Cooperation of CCAAT Box/Enhancer-binding Protein β (C/EBPβ) and Co-activator p300. J Biol Chem. 2016 Dec 9;291(50):26098-26108.