LJH-685

LJH685 is a potent , specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50 of 4 to 13 nM.IC50 value: 4 to 13 nM [1]Target: RSKin vitro: LJH685 efficiently inhibits RSK activity in cells. LJH685 RSK inhibition correlates with antiproliferative effects in MAPK pathway-dependent cancer cell lines only in anchorage-independent growth setting. The EC 50 values of LJH685 is 0.73 and 0.79 μM in MDA-MB-231 and H358. [1]

Signaling Pathways >> MAPK/ERK Pathway >> Ribosomal S6 Kinase (RSK)

Research Areas >> Cancer

[1]. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.

[2]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.

[3]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.

BI-D1870 | CMK | PF-4708671 | LY-2584702 tosylate salt | BIX 02565 | AT7867 | Pluripotin | Quercitrin | A-196 | LJI308 | AT13148 | Carnosol