LJH685

LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively.

Product information

CAS Number: 1627710-50-2

Molecular Weight: 381.42

Formula: C22H21F2N3O

Chemical Name: 2, 6-difluoro-4-{4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl}phenol

Smiles: CN1CCN(CC1)C1C=CC(=CC=1)C1=CC=NC=C1C1=CC(F)=C(O)C(F)=C1

InChiKey: IKUFKDGKRLMXEX-UHFFFAOYSA-N

InChi: InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 31 mg/mL (81.28 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC50s of 0.73 and 0.79 μM, respectively. LJH685 (0.1-10 μM; 4 hours) efficiently reduces phosphorylation of YB1 at submicromolar concentrations and causes nearly complete inhibition at higher concentrations.

References:

1. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.
2. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.
3. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.

Products are for research use only. Not for human use.