| Arylquin 1potent secretagogue of the tumor suppressor protein prostate apoptosis response-4 (Par-4) |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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| Cas No. | 1630743-73-5 | SDF | Download SDF |
| 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 | ||
| Formula | C17H16FN3 | M.Wt | 281.3 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
