Home PI3K/Akt/mTOR S6 Kinase inhibitor LJH685 For research use only.

LJH685

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

LJH685 Chemical Structure

LJH685 Chemical Structure

CAS: 1627710-50-2

Selleck's LJH685 has been cited by 7 Publications

1 Customer Review

Purity & Quality Control

Batch: S787001 Ethanol] 20 mg/mL] false] DMSO] 10 mg/mL] false] Water] Insoluble] false Purity: 99.86%
99.86

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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
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]
Kinase Assay 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 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.

Chemical Information & Solubility

Molecular Weight 381.42 Formula

C22H21F2N3O
CAS No. 1627710-50-2 SDF Download LJH685 SDF
Smiles CN1CCN(CC1)C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 20 mg/mL

DMSO : 10 mg/mL ( (26.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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