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LJI308

CAT: 0804-HY-19713-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-19713-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
RSK2; RSK3

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CatalogName
B6043-100LJI308

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