LJI308

LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation[1][2].

Product Specifications

CAS Number

[1627709-94-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ribosomal S6 Kinase (RSK) ; YB-1

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LJI308.html

Purity

99.07

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

OC1=C(C=C(C=C1F)C2=C(C=CN=C2)C3=CC=C(C=C3)N4CCOCC4)F

Molecular Formula

C21H18F2N2O2

Molecular Weight

368.38

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]Lettau K, et al. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021;109 (2) :567-580.|[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]Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6 (24) :20570-20577.