Description
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 . 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.
Product information
CAS Number: 1630743-73-5
Molecular Weight: 281.33
Formula: C17H16FN3
Chemical Name: 3-(2-fluorophenyl)-N7,N7-dimethylquinoline-2,7-diamine
Smiles: CN(C)C1=CC2N=C(N)C(=CC=2C=C1)C1=CC=CC=C1F
InChiKey: RHAQINSYYSNKKI-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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