Yangonin

Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC₅₀ and a K_i of 1.79 μM and 0.72 μM, respectively. IC50 & Target: IC50: 1.79±0.53 μM (hCB1 receptor), >10 μM (hCB2 receptor)^[1]
Ki: 0.72±0.21 μM (hCB1 receptor), >10 μM (hCB2 receptor)^[1]
RelA/p65^[2] In Vitro: Yangonin is one of the six major kavalactones found in Piper methysticum.Yangonin potently inhibits NF-κB activation through suppression of the transcriptional activity of the RelA/p65 subunit of NF-κB. Yangonin significantly inhibits the induced expression of the NF-κB-reporter gene. However, Yangonin does not interfere with TNF-α-induced inhibitor of κBα (IκBα) degradation, p65 nuclear translocation, and DNA-binding activity of NF-κB. Yangonin inhibits not only the induced NF-κB activation by overexpression of RelA/p65, but also transactivation activity of RelA/p65. Yangonin does not inhibit TNF-α-induced activation of p38, but it significantly impairs activation of ERK 1/2 and stress-activated protein kinase/JNK^[2].