950244-33-4

JS6 is a Bcl3 inhibitor, and inhibits Bcl3-NF-kB1 binding. JS6 inhibits tumor cell growth in vitro and in vivo[1].

JS6 is a Bcl3:NF-kB p50 protein-protein interaction (PPI) inhibitor th at effectively suppresses Bcl3-dependent intracellular NF-kB activity (IC50 = 45/159 nM using Bcl3-overexpressing MDA-MB-231/HEK293; IC50 = 710 nM using HEK293 overexpressing Bcl3 and NF-kB p52). JS6 prevents enhanced MDA-MB-231 migration upon Bcl3 overexpression in cultures (IC50 = 310 nM)and effectively suppresses primary tumor growth as well as secondary tumor colonisation in vivo (3.5-10 mg/kg/d i.p. mice with MDA-MB-436 or 4T1.2 murine carcinoma xenograft) without overt systemic toxicity.

[1] Soukupová J, et al. The Discovery of a Novel Antimetastatic Bcl3 Inhibitor. Mol Cancer Ther. 2021;20(5):775-786. DOI:10.1158/1535-7163.MCT-20-0283