| Chemical Properties | Back Directory | [Boiling point ]
441.4±40.0 °C(Predicted) | [density ]
1.241±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
A crystalline solid | [pka]
7.49±0.50(Predicted) | [color ]
white to yellow to light brown | [InChI]
1S/C17H16FN3/c1-21(2)12-8-7-11-9-14(17(19)20-16(11)10-12)13-5-3-4-6-15(13)18/h3-10H,1-2H3,(H2,19,20) | [InChIKey]
RHAQINSYYSNKKI-UHFFFAOYSA-N | [SMILES]
NC1=NC2=CC(N(C)C)=CC=C2C=C1C3=CC=CC=C3F |
| Hazard Information | Back Directory | [Uses]
Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, targets vimentin to induce Par-4 secretion. Arylquin 1 induces non-apoptotic cell death in cancer cells through the induction of lysosomal membrane permeabilization (LMP)[1]. | [Biological Activity]
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]. | [storage]
Store at -20°C | [References]
[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. |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|