CAS NO: | 1630743-73-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Storage | Store at -20°C |
M.Wt | 281.3 |
Cas No. | 1630743-73-5 |
Formula | C17H16FN3 |
Solubility | Soluble in DMSO |
Chemical Name | 3-(2-fluorophenyl)-N7,N7-dimethyl-2,7-quinolinediamine |
Canonical SMILES | CN(C)C1=CC=C2C(N=C(N)C(C3=CC=CC=C3F)=C2)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.