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LJH685

LJH685
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Purity:99.78%
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LJH685

Catalog No. T6877Cas No. 1627710-50-2
LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$33In Stock
2 mg$45In Stock
5 mg$81In Stock
10 mg$147In Stock
25 mg$296In Stock
50 mg$471In Stock
100 mg$688In Stock
1 mL x 10 mM (in DMSO)$93In Stock
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Product Introduction

Bioactivity
Description
LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 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]
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 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)
Chemical Properties
Molecular Weight381.42
FormulaC22H21F2N3O
Cas No.1627710-50-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 71 mg/mL (186.1 mM)
Ethanol: 16 mg/mL (41.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.6218 mL13.1089 mL26.2178 mL131.0891 mL
5 mM0.5244 mL2.6218 mL5.2436 mL26.2178 mL
10 mM0.2622 mL1.3109 mL2.6218 mL13.1089 mL
20 mM0.1311 mL0.6554 mL1.3109 mL6.5545 mL
DMSO
1mg5mg10mg50mg
50 mM0.0524 mL0.2622 mL0.5244 mL2.6218 mL
100 mM0.0262 mL0.1311 mL0.2622 mL1.3109 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
1 Enter information below:
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