Indole-3-carbinol

Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1). IC50 & Target: Aryl hydrocarbon receptor (AhR)^[2], NF-κB^[2], WWP1^[3] In Vitro: It is found that Indole-3-carbinol (I3C) inhibits the proliferation of THP-1 cells in a dose- and time dependent manner with minimal toxicity over normal monocytes. The AhR target genes (CYP1A1, IL1β) are overexpressed upon Indole-3-carbinol treatment (p<0.05 to p<0.001). The antiproliferative effects of Indole-3-carbinol are in association with programing cell death. Indole-3-carbinol downregulates BCL2 and upregulates FasR in THP-1 cells (p<0.05 to p<0.001). G1 cell cycle arrest is also observed using flow cytometry. G1-acting cell cycle genes (P21, P27 and P53) are overexpressed (p<0.05 to p<0.001), while CDK2 is downregulated upon Indole-3-carbinol treatment (p<0.01 to p<0.001)^[1].Indole-3-carbinol suppresses NF-κB activity and stimulates the p53 pathway in pre-B acute lymphoblastic leukemia cells^[2].