Structural basis for the activity of the RSK-specific inhibitor, SL0101

The mitogen‐activated protein kinase signaling pathways: role in megakaryocyte differentiation

“…In particular, in K562 cells, sequential activation of ERK, RSK1 and NF-jB has been shown to mediate PMA-induced megakaryocytic differentiation [87]. However, a recent report using the RSK inhibitor, SL0101, showed that RSK is not required for MK differentiation from mouse progenitors cells [75,88] thereby emphasizing the importance of confirming results in primary cells.…”

The p90 RSK Family Members: Common Functions and Isoform Specificity

“…However, SL-0101 has shown a much higher EC 50 in vivo, a fact that may be of concern to specificity. When used in culture, this compound impaired the growth of MCF-7 breast cancer cells without effect on normal MCF-10A breast epithelial cells, suggesting that it may specifically target cancer cells that rely on RSK for their growth (48). However, we have found that this inhibitor promotes the invasive behavior of NSCLC cells (unpublished data).…”

“…When tested against a panel of 70 kinases, it was shown to target RSK1 and RSK2 in the nanomolar range (IC 50 for RSK2, 90 nmol/L at 10 mmol/L ATP; ref. 48) while having no significant activity against other tested AGC kinases (19). However, SL-0101 has shown a much higher EC 50 in vivo, a fact that may be of concern to specificity.…”

Cytotoxic polyphenols against breast tumor cell in Smilax china L.

“…Because flavanoids and stilbenoids are polyphenol-rich on the basis of our extracting experiments and their known anti-tumor activity (Li et al, 2007;Smith et al, 2007;Xu et al, 2008), we proposed that polyphenols in this species would be potential antitumor bioactive compounds.…”