您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Dequalinium Chloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Dequalinium Chloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dequalinium Chloride图片
CAS NO:522-51-0
规格:98%
分子量:527.57
包装与价格:
包装价格(元)
50mg电议
250mg电议

产品介绍
anti-tumor agent and PKC inhibitor
CAS:522-51-0
分子式:C30H40N4.2Cl
分子量:527.57
纯度:98%
存储:Store at -20°C

Background:

Dequalinium Chloride (DECA) is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM [1][3].
Protein kinase C (PKC) is a monomeric Ca2+- and phospholipid-dependent Ser/Thr protein kinases, it plays a critical role in growth factor-activated signaling and malignant transformation [1].
DECA is an anti-tumor agent and PKC inhibitor. It is selectively accumulated and retained within the mitochondria of carcinoma cells where it blocked mitochondrial enzymes which can then disrupt cellular energy production, eventually resulting in cell death [2]. Dequalinium is a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Dequalinium blocked angiotensin II-evoked K+ loss with an IC50 value of 1.5 μM and also inhibited 125I - monoiodoapamin binding with Ki of 1.1 μM [3].
DECA, as a mitochondrial poison, is an agent with capable of potentiating the effects of tumor necrosis factor against ovarian cancer cell lines. DECA treatment can prolong animal survival in mice bearing the PA-1 intraperitoneal ovarian carcinoma xenograft. Single agent DECA increased animal survival by 37% whereas human TNF increased survival by 12% in those animals treated 3 days post tumor injection. DECA/TNF enhanced animal survival by 45% in treated animals [4].
参考文献:
[1]. Rotenberg SA, Sun XG. Photoinduced inactivation of protein kinase C by dequalinium identifies the RACK-1-binding domain as a recognition site. J Biol Chem, 1998, 273(4): 2390-2395.
[2]. Manetta A, Emma D, Gamboa G, et al. Failure to enhance the in vivo killing of human ovarian carcinoma by sequential treatment with dequalinium chloride and tumor necrosis factor. Gynecol Oncol, 1993, 50(1): 38-44.
[3]. Castle NA, Haylett DG, Morgan JM, et al. Dequalinium: a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Eur J Pharmacol, 1993, 236(2): 201-207.
[4]. Manetta A, Emma D, Fuchtner C, et al. Effect of recombinant human tumor-necrosis-factor-alpha and dequalinium chloride on human ovarian-cancer cell-lines in-vitro. Int J Oncol, 1993, 3(1): 127-33.