product name Dequalinium Chloride
Description: Dequalinium Chloride 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. Dequalinium 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. Dequalinium is a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle.
References: Gynecol Oncol. 1993;50:38-44; Eur J Pharmacol. 1993;236:201-7; Proc Natl Acad Sci U S A. 1987;84:5444-8.
527.57
Formula
C30H40N4.2Cl
CAS No.
522-51-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Dequalinium chloride (DECA) is a cationic, lipophilic compound with structure similar to the dye rhodamine 123. DECA is selectively accumulated and retained within the mitochondria of carcinoma cells where it acts as a mitochondrial poison by blocking mitochondrial enzymes which can then disrupt cellular energy production, eventually resulting in cell death. Dequalinium Chloride is a blocker of ganglionic transmission (EC50 = 2 μM). Dequalinium is a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Dequalinium blocks angiotensin II-evoked K+ loss with an IC50 of 1.5 μM and also inhibited125I – monoiodoapamin binding with Ki of 1.1 μM. Dequalinium produces a rapid and reversible inhibition of the slow apamin-sensitive component of the afterhyperpolarization (AHP) which follows a single action potential in cultured rat sympathetic neurons. Dequalinium Chloride (DECA) is a dicationic lipophilic PKC inhibitor. When exposed to UV light, DECA covalently binds to and irreversibly inhibits PKCα and PKCβ. Kinase Assay: Cell Assay: DECA, as a mitochondrial poison, is an agent with capable of potentiating the effects of tumor necrosis factor against ovarian cancer cell lines. |
|---|---|
| In Vivo | In mice bearing bladder MB49 tumors, Dequalinium chloride (2 mg/kg/d, i.p.) displays anticarcinoma activity with T/C of 210%. |
| Animal model | Mice bearing bladder MB49 tumors |
| Formulation & Dosage | Dissolved in water using a bath sonicator; 2 mg/kg; i.p. injection |
| References | Gynecol Oncol. 1993 Jul;50(1):38-44; Eur J Pharmacol. 1993 May 19;236(2):201-7; Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8. |
