Merck, SML3261-5MG, JS6

Biochem/physiol Actions
Bcl3:NF-kB p50 protein-protein interaction (PPI) inhibitor with anti-metastatic efficacy in cultures and in vivo.
JS6 is a Bcl3:NF-kB p50 protein-protein interaction (PPI) inhibitor that 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.