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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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