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LJI308

🥰Excellent
Catalog No. T6878Cas No. 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.

LJI308

LJI308

🥰Excellent
Purity: 99.73%
Catalog No. T6878Cas No. 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.
Pack SizePriceAvailabilityQuantity
1 mg$38In Stock
5 mg$81In Stock
10 mg$98In Stock
25 mg$225In Stock
50 mg$351In Stock
100 mg$540In Stock
1 mL x 10 mM (in DMSO)$89In Stock
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Purity:99.73%
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Product Introduction

Bioactivity
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)
Chemical Properties
Molecular Weight368.38
FormulaC21H18F2N2O2
Cas No.1627709-94-7
SmilesOc1c(F)cc(cc1F)-c1cnccc1-c1ccc(cc1)N1CCOCC1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 50 mg/mL (135.73 mM), Heating is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7146 mL13.5729 mL27.1459 mL135.7294 mL
5 mM0.5429 mL2.7146 mL5.4292 mL27.1459 mL
10 mM0.2715 mL1.3573 mL2.7146 mL13.5729 mL
20 mM0.1357 mL0.6786 mL1.3573 mL6.7865 mL
50 mM0.0543 mL0.2715 mL0.5429 mL2.7146 mL
100 mM0.0271 mL0.1357 mL0.2715 mL1.3573 mL

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