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Arylquin 1
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。
Arylquin 1图片
CAS NO:1630743-73-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Arylquin 1 是一种前列腺凋亡反应 4 (Par-4) 促分泌素,靶向波形蛋白以诱导 Par-4 分泌。 Arylquin 1 通过诱导溶酶体膜透化 (LMP) 诱导癌细胞中的非凋亡性细胞死亡。
Cas No.1630743-73-5
化学名3-(2-fluorophenyl)-N7,N7-dimethyl-2,7-quinolinediamine
Canonical SMILESCN(C)C1=CC=C2C(N=C(N)C(C3=CC=CC=C3F)=C2)=C1
分子式C17H16FN3
分子量281.3
溶解度DMSO: 20 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Arylquin 1 is a potent secretagogue of the tumor suppressor protein prostate apoptosis response-4 (Par-4).

Par-4 is ubiquitously expressed in normal cells and tissues, but it is inactivated, downregulated or mutated in several types of cancers. Par-4 can selectively induce cancer cell apoptosis but not normal cells. Both intracellular and secreted Par-4 have a role in apoptosis induction by caspase-dependent mechanisms.

In vitro: Previous study showed that Arylquin 1 produced a dose-dependent secretion in MEF cells and also induced robust secretion of Par-4 in normal or immortalized human cells but failed to induce the secretion of Par-4 in various lung tumor cells. Moreover, it was found that Brefeldin A, which blocked anterograde endoplasmic reticulum–Golgi traffic, could inhibit basal and Arylquin 1–inducible Par-4 secretion, indicating that Arylquin 1 regulated Par-4 secretion through the classical secretory pathway. In addition, cells treated with Arylquin 1 showed neither Par-4 co-immunoprecipitation nor colocalization with vimentin, suggesting that Arylquin 1 could displace Par-4 from vimentin. This action of Arylquin 1 was not associated with inhibition of vimentin expression, demonstrating that Arylquin 1 might cause conformational changes in vimentin to block its ability to bind and sequester Par-4 [1].

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

Clinical trial: Up to now, Arylquin 1 is still in the preclinical development stage.

Reference:
[1] Burikhanov R et al.  Arylquins target vimentin to trigger Par-4 secretion for tumor cell apoptosis. Nat Chem Biol. 2014 Nov;10(11):924-6.