Dequalinium Chloride

Catalog No.S4066

Molecular Weight(MW): 527.57

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.

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Biological Activity

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.

Targets

PKC ^[1]

7 μM-18 μM

In vitro

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). ^[1] 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 K_i of 1.1 μM. ^[2] 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 neurones. ^[3] Dequalinium Chloride (DECA) is a dicationic lipophilic PKC inhibitor. When exposed to UV light, DECA covalently binds to and irreversibly inhibits PKCα and PKCβ. ^[4]

In vivo

In mice bearing bladder MB49 tumors, Dequalinium chloride (2 mg/kg/d, i.p.) displays anticarcinoma activity with T/C of 210%. ^[5]

Protocol

Animal Research: ^[5]	+ Expand Animal Models: Mice bearing bladder MB49 tumors Formulation: Dissolved in water using a bath sonicator Dosages: 2 mg/kg/d Administration: i.p. (Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	0.025 mg/mL (0.04 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Dequalinium Chloride SDF

Molecular Weight	527.57
Formula	C₃₀H₄₀N₄.2Cl
CAS No.	522-51-0
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01125410	Completed	Bacterial Vaginosis	Medinova AG	January 2007	Phase 3
NCT01125410	Completed	Bacterial Vaginosis	Medinova AG	January 2007	Phase 3

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PKC Signaling Pathway Map

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