BI-D1870 is a potent and specific RSK inhibitor (the p90 ribosomal S6 kinase), which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10–30 nM. BI-D1870 exhibited a dose-responsive antiproliferative effect on OSCC cells with relative sparing of normal human oral keratinocytes. The compound inhibited the downstream RSK target YB-1 and caused apoptosis. In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. BI-D1870 may be of useful in oral squamous cell carcinoma therapy.
安全信息
Storage condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).