| Description | Dequalinium chloride (Decabis) , a topical bacteriostat, is a selective blocker of apamin-sensitive K+ channels. It is used in wound dressings and mouth infections and may also have antifungal action, but may cause skin ulceration. |
| In vitro | Dequalinium chloride可有效抑制骨骼肌中的烟碱响应以及蜂毒明肽敏感的肝细胞中的钾离子通道。此外,它还是是神经节传导阻滞剂（EC50：2 μM）。作为阳离子亲脂性PKC抑制剂 ,Dequalinium chloride与染料Rhodamine 123具有相似结构。Dequalinium chloride在UV光照射下可以共价结合的方式不可逆地抑制PKCα/β。Dequalinium chloride在肿瘤细胞的线粒体中选择性积累,通过阻断线粒体酶产生线粒体毒性,从而破坏细胞能量产生,致使细胞死亡。Dequalinium抑制125I- monoiodoapamin的结合（Ki：1.1 μM）,防止钾离子损失（血管紧张素II诱发,IC50：1.5 μM）。在培养的大鼠交感神经神经元中,Dequalinium能快速可逆地抑制缓慢蜂毒明肽敏感的后超极化(AHP)成分,接着会产生单一的一个动作电位。 |
| In vivo | 在负荷膀胱MB49肿瘤的小鼠体内, Dequalinium chloride（2 mg/kg/day i.p）产生抗癌作用,T/C为210%. |
| Target activity | PKC:7 μM-18 μM |
| Synonyms | Dequafungan, 地喹氯铵, Danical, Decabis |
| molecular weight | 527.59 |
| Molecular formula | C30H40Cl2N4 |
| CAS | 522-51-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: Insoluble H2O: 3.3mg/ml（6.3mM）, Sonication is recommended. |
| References | 1. Manetta A, et al. Gynecol Oncol, 1993, 50(1), 38-44. 2. Castle NA, et al. Eur J Pharmacol, 1993, 236(2), 201-207. 3. Dunn PM, et al. Eur J Pharmacol, 1994, 252(2), 189-194. 4. Rotenberg SA, et al. J Biol Chem, 1998, 273(4), 2390-2395. 5. Weiss MJ, et al. Proc Natl Acad Sci U S A. 1987, 84(15), 5444-5448. |