LJI308

$180$1,980

Products Details

Product Description

– 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].

Web ID

– HY-19713

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C21H18F2N2O2

References

– [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.

CAS Number

– 1627709-94-7

Molecular Weight

– 368.38

Compound Purity

– 99.21

SMILES

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 25 mg/mL (ultrasonic)

Target

– Ribosomal S6 Kinase (RSK);YB-1

Isoform

– RSK1;RSK2;RSK3

Pathway

– Cell Cycle/DNA Damage;MAPK/ERK Pathway

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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