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LJH685 Sale

(Synonyms: 2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚) 目录号 : GC16039

An inhibitor of RSKs

LJH685 Chemical Structure

Cas No.:1627710-50-2

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5mg
¥620.00
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25mg
¥2,121.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

IC50: 6 nM, 5 nM and 4 nM for the biochemical activities of RSK1, RSK2, and RSK3, respectively

LJH685 is a RSK (p90 ribosomal S6 kinase) inhibitor.

The p90 ribosomal S6 kinase (RSK) family of serine/threonine kinases is found to be expressed in a variety of cancers and its substrate phosphorylation has been implicated in direct regulation of cell proliferation, cell survival, as well as cell polarity.

In vitro: In a previous study, the structural analysis results confirmed the binding of LJH685 to the RSK2 N-terminal kinase ATP-binding site, which suggested that the inhibitor LJH685 adopted an unusual nonplanar conformation that explained its excellent selectivity for RSK family kinases. In addition, LJH685 and it analog LJI308 could efficiently inhibit RSK activity in vitro and in cells. Moreover, in a subset of examined cell lines, the cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 were found to be closely associate with the inhibition of cell growth in an anchorage-independent growth setting [1].

In vivo: So far, there is no animal in vivo data reported for LJH685.

Clinical trial: Up to now, LJH685 is still in the preclinical development stage.

Reference:
[1] Aronchik I, Appleton BA,Basham SE,Crawford K,Del Rosario M,Doyle LV,Estacio WF,Lan J,Lindvall MK,Luu CA,Ornelas E,Venetsanakos E,Shafer CM,Jefferson AB.  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.

Chemical Properties

Cas No. 1627710-50-2 SDF
别名 2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚
化学名 2,6-difluoro-4-(4-(4-(4-methylpiperazin-1-yl)phenyl)pyridin-3-yl)phenol
Canonical SMILES OC1=C(F)C=C(C2=C(C3=CC=C(N4CCN(C)CC4)C=C3)C=CN=C2)C=C1F
分子式 C22H21F2N3O 分子量 381.42
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.125 mg/ml,Ethanol: 2.5 mg/ml 储存条件 Store at -20°C
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1 mM 2.6218 mL 13.1089 mL 26.2178 mL
5 mM 0.5244 mL 2.6218 mL 5.2436 mL
10 mM 0.2622 mL 1.3109 mL 2.6218 mL
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