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SC-514, a Selective Inhibitor of IKKβ Attenuates RANKL-induced Osteoclastogenesis and NF-κB Activation

SC-514, a Selective Inhibitor of IKKβ Attenuates RANKL-induced Osteoclastogenesis and NF-κB Activation

Qian Liu, Huafei Wu, Shek Man Chim, Lin Zhou, Jinmin Zhao, Haotian Feng, Qingli Wei, Qing Wang, Ming H Zheng, Ren Xiang Tan, Qiong Gu, Jun Xu, Nathan Pavlos, Jennifer Tickner, Jiake Xu

Biochem Pharmacol. 2013 Dec 15;86(12):1775-83.

PMID: 24091016

Abstract:

The RANKL-induced NF-κB signaling pathway is essential for osteoclastogenesis. This study aims to identify specific inhibitors targeting NF-κB signaling pathway, which might serve as useful small molecule inhibitors for the treatment and alleviation of osteoclast-mediated bone lytic diseases. By screening for compounds that selectively inhibit RANKL-induced NF-κB activation in RAW264.7 cells as monitored by luciferase reporter gene assay, we identified SC-514, a specific inhibitor of IKKβ, as a candidate compound targeting osteoclastogenesis. SC-514 dose-dependently inhibits RANKL-induced osteoclastogenesis with an IC50 of <5μM. At high concentrations, SC-514 (≥12.5μM) induced apoptosis and caspase 3 activation in RAW264.7 cells. Moreover, SC-514 specifically suppressed NF-κB activity owing to delayed RANKL-induced degradation of IκBα and inhibition of p65 nuclear translocation. Taken together, our results indicate that SC-514 impairs RANKL-induced osteoclastogenesis and NF-κB activation. Thus, targeting IKKβ by SC-514 presents as a potential treatment for osteoclast-related disorders such as osteoporosis and cancer-induced bone loss.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP354812172	SC-514		354812-17-2	Price

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