Home TGF-beta/Smad PKC inhibitor Dequalinium Chloride

Dequalinium Chloride

Catalog No.S4066

For research use only.

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 Chloride Chemical Structure

CAS No. 522-51-0

Selleck's Dequalinium Chloride has been cited by 2 Publications

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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 Ki 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 (from reference)

Animal Research:

[5]
  • Animal Models: Mice bearing bladder MB49 tumors
  • Dosages: 2 mg/kg/d
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 527.57
Formula

C30H40N4.2Cl
CAS No. 522-51-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=[N+](C2=CC=CC=C2C(=C1)N)CCCCCCCCCC[N+]3=C(C=C(C4=CC=CC=C43)N)C.[Cl-].[Cl-]

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