LJH685 是一种选择性，ATP-竞争性的RSK抑制剂, 抑制 RSK1/2/3 生物活性，IC50为 6、5、4 nM。

LJH685 is an effective pan-RSK inhibitor for RSK1/2/3 (IC50: 6/5/4 nM).

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]

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 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)

1627710-50-2

C22H21F2N3O

381.427

DMSO:71 mg/mL (186.1 mM)
Ethanol:16 mg/mL (41.9 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years