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LJI308

Catalog No. T6878 CAS 1627709-94-7

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

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LJI308, CAS 1627709-94-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 225.00
50 mg	In stock	$ 351.00
100 mg	In stock	$ 540.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 99.73%

Purity: 98.86%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.
Targets&IC50	RSK3:13 nM, RSK2:4 nM, RSK1:6 nM
In vitro	In MDA-MB-231 and H358 cells, LJI308 blocks cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 with EC50 of 0.2–0.3 μM, and thus inhibits cell growth. [1] In TNBC HTRY-LT cells, LJI308 also suppresses cell growth correlative with YB-1 inhibition. [2]
Kinase Assay	Inhibition of RSK1, RSK2, and RSK3 activity: Enzymatic activity of RSK isoforms 1, 2, and 3 is assessed using recombinant full-length RSK protein. RSK1 (1 nM), RSK2 (0.1 nM), or RSK3 (1 nM) is allowed to phosphorylate 200 nM peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1- 5 μM, RSK2- 20 μM, RSK3- 10 μM) and appropriate dilutions of RSK inhibitors in 50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.1% BSA Fraction V, 0.01% Tween-20. After 150 min at room temperature, the reaction is stopped with 60 mM EDTA and extent of peptide phosphorylation was determined using an anti-phospho-AKT substrate antibody and AlphaScreen reagents as described by the manufacturer.
Cell Research	Cell growth under attached conditions is assessed by plating 1000 cells per well on 96-well tissue culture-treated plates in cell growth medium. Appropriate dilutions of compound are 4 added medium above cells and cell growth was assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer’s directions. (Only for Reference)

Molecular Weight	368.38
Formula	C21H18F2N2O2
CAS No.	1627709-94-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 50 mg/mL (135.73 mM), Heating is recommended.

References and Literature

1. Aronchik I, et al. Mol Cancer Res. 2014, 12(5), 803-812. 2. Davies AH, et al. Oncotarget. 2015, 6(24), 20570-205777.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Stem Cell Differentiation Compound Library Anti-Cancer Compound Library Anti-Liver Cancer Compound Library Antidepressant Compound Library Metabolism Compound Library Anti-Lung Cancer Compound Library Reprogramming Compound Library Anti-Ovarian Cancer Compound Library Glycolysis Compound Library

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Keywords

LJI308 1627709-94-7 MAPK PI3K/Akt/mTOR signaling S6 Kinase viability Ribosomal S6 Kinase (RSK) stimulation phosphorylation inhibit mutation Inhibitor breaks double-strand cancer LJI-308 LJI 308 S6K inhibitor

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