LJH685

LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively[1].

Product Specifications

CAS Number

[1627710-50-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Ribosomal S6 Kinase (RSK)

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LJH685.html

Concentration

10mM

Purity

99.64

Solubility

DMSO : ≥ 31 mg/mL

Smiles

OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F

Molecular Formula

C22H21F2N3O

Molecular Weight

381.42

Precautions

H302, H315, H319, H335

References & Citations

[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.|[4]My-My Huynh, et al. RSK2: a promising therapeutic target for the treatment of triple-negative breast cancer. Expert Opin Ther Targets. 2020 Jan;24 (1) :1-5.