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.
Molecular cancer therapeutics, 20(5), 775-786 (2021-03-03)
The development of antimetastatic drugs is an urgent healthcare priority for patients with cancer, because metastasis is thought to account for around 90% of cancer deaths. Current antimetastatic treatment options are limited and often associated with poor long-term survival and
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