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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $225 | In Stock | |
50 mg | $351 | In Stock | |
100 mg | $540 | In Stock | |
1 mL x 10 mM (in DMSO) | $89 | In Stock |
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 |
Smiles | Oc1c(F)cc(cc1F)-c1cnccc1-c1ccc(cc1)N1CCOCC1 |
Relative Density. | no data available |
Storage | Powder: -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
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