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LJI308
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LJI308图片
CAS NO:1627709-94-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
LJI308 是泛RSK抑制剂,对 RSK1、RSK2 和 RSK3 的IC50分别为 6、4 和 13 nM。它抑制辐照、EGF 处理和表达 KRas 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。

产品描述

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

体外活性

In MDA-MB-231 and H358 cells, LJI308 blocks cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 with EC50 of 0.2–0.3 μM, and thus inhibits cell growth. [1] In TNBC HTRY-LT cells, LJI308 also suppresses cell growth correlative with YB-1 inhibition. [2]

激酶实验

Inhibition of RSK1, RSK2, and RSK3 activity: Enzymatic activity of RSK isoforms 1, 2, and 3 is assessed using recombinant full-length RSK protein. RSK1 (1 nM), RSK2 (0.1 nM), or RSK3 (1 nM) is allowed to phosphorylate 200 nM peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1- 5 μM, RSK2- 20 μM, RSK3- 10 μM) and appropriate dilutions of RSK inhibitors in 50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.1% BSA Fraction V, 0.01% Tween-20. After 150 min at room temperature, the reaction is stopped with 60 mM EDTA and extent of peptide phosphorylation was determined using an anti-phospho-AKT substrate antibody and AlphaScreen reagents as described by the manufacturer.

细胞实验

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 4 added medium above cells and cell growth was assessed after 72 hrs by addition of CellTiter Glo reagent according to manufacturer’s directions. (Only for Reference)

Cas No.

1627709-94-7

分子式

C21H18F2N2O2

分子量

368.384

储存和溶解度

H2O:Insoluble
DMSO:10 mg/mL,warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years