2016年3月10日星期四

LJH-685|CAS 1627710-50-2|RSK inhibitor|DC Chemicals

LJH-685|CAS 1627710-50-2|RSK inhibitor|DC Chemicals

LJH685 is a selective and potent RSK inhibitor.

Product Name: LJH-685|Cat No.:DC8811|CAS: 1627710-50-2|Other names: LJH-685,LJH 685,LJH685|MW: 381.42|C22H21F2N3O

LJH685 is a selective and potent RSK inhibitor. Structural analysis confirms binding of LJH685 to the RSK2 N-terminal kinase ATP-binding site and reveals that the inhibitor adopts an unusual nonplanar conformation that explains its excellent selectivity for RSK family kinases. LJH685 and LJI308 efficiently inhibit RSK activity in vitro and in cells. Furthermore, cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 correlate closely with inhibition of cell growth, but only in an anchorage-independent growth setting, and in a subset of examined cell lines. Thus, RSK inhibition reveals dynamic functional responses among the inhibitor-sensitive cell lines, underscoring the heterogeneous nature of RSK dependence in cancer.

For research only, not for human use!

没有评论:

发表评论