LJH685

Catalog No.S7870

LJH685 Chemical Structure

Molecular Weight(MW): 381.42

LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.

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1 Customer Review

  • In (E), single (left panel) and double resistant (right panel) SKMel28 cells were treated with vemurafenib, the RSK inhibitor LJH-685 or the combination.

    Oncotarget, 2017, 8(22):35761-35775. LJH685 purchased from Selleck.

Purity & Quality Control

Choose Selective S6 Kinase Inhibitors

Biological Activity

Description LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.
Targets
RSK3 [1]
(Cell-free assay)
RSK2 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
4 nM 5 nM 6 nM
In vitro

LJH685 modulates YB1 phosphorylation by potently and selectively inhibiting RSK in cells. In MAPK pathway–dependent cancer cell lines, LJH685 shows antiproliferative effects, and causes cell-cycle regulation and apoptosis induction. [1]

Protocol

Kinase Assay:[1]
+ Expand

Inhibition of RSK1, RSK2, and RSK3 activity:

Enzymatic activity of RSK isoforms 1, 2, and 3 (PV4049, PV4051, and PV3846) is assessed using recombinant full-length RSK protein. RSK1 (1 nmol/L), RSK2 (0.1 nmol/L), or RSK3 (1 nmol/L) is allowed to phosphorylate 200 nmol/L peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1, 5 μmol/L; RSK2, 20 μmol/L; and RSK3, 10 μmol/L) and appropriate dilutions of RSK inhibitors.
Cell Research:[1]
+ Expand
  • Cell lines: Calu6, NCI-H2122, NCI-H358, NCI-H727, NCI-H2087, SW620, SW480, HT29, Capan-2, MiaPaCa2, SW1990, Panc02.03, MDA-MB-231, A375, G361, Colo205, Malme3M, WM1799, WM983B and WM266-4 cells
  • Concentrations: ~100 μM
  • Incubation Time: 72 h
  • Method: 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 added medium above cells and cell growth is assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer’s directions.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.25 mM)
Ethanol 20 mg/mL (52.43 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 381.42
Formula

C22H21F2N3O

CAS No. 1627710-50-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID