Quinacrine Inhibitor

Quinacrine Inhibitor [NBP2-29385]

Quinacrine Inhibitor [NBP2-29385] - Evaluation of inhibitory activity of quinacrine. TLR9/NF-kB/SEAPorter™ HEK 293 and TLR2/NF-kB/SEAPorter™ HEK 293 cells were plated in 96-well plates at 5x10^4 cells/well for 16 h. Cells were preincubated with different concentrations of quinacrine (0.05, 0.1, 0.5, 1, 5 and 10 uM) for 30 min. Cell were then stimulated with 10 ug/ml CpG [A] or 20 ng/ml MALP-2 [B] for 24 h. Secreted alkaline phosphatase (SEAP) was analyzed using SEAPorter™ Assay Kit

Quinacrine Inhibitor [NBP2-29385] - TLR9/NF-kB/SEAPorter™ HEK 293 cells were plated in 96-well plates at 5x10^4 cells/well for 16 h. Cells were preincubated with various concentrations of quinacrine for 30 min, followed by stimulation with 10 ug/ml CpG for 24 h. SEAP was analyzed using SEAPorter™ Assay Kit. Dose-responsive percent inhibition of each sample well was calculated to yield the quinacrine IC50 value.

Quinacrine Inhibitor Summary

• Immunogen: CAS Number 69-05-6
  Empirical Formula (Hill Notation) C23H30ClN3O. 2HCl
  Molecular Weight 472.88
• Details of Functionality: Endosomal toll-like receptor inhibitor (antagonist); Inhibitor of endosomal acidification on which functional activity of endosomal TLRs (particularly TLR9 and TLR3) is dependent.

Applications/Dilutions

• Application Notes: Assay>=90%

Packaging, Storage & Formulations

• Storage: Store at 4C. Do not freeze.
• Buffer: Form : Yellow Solid (Powder)
  Solubility:Deionized water

Alternate Names for Quinacrine Inhibitor

• 1-2-bromophenyl-5-3-methylphenyl triazole-4-carboxylic acid
• 6-Chloro-9-4-diethylamino-1-methylbutylamino-2-methoxyacridine dihydrochloride
• Atebrin dihydrochloride
• C23H30ClN3O-2HCl
• Mepacrine dihydrochloride
• Quinacrine dihydrochloride

Background

Quinacrine is a weak base which can partition into acidic vesicles such as endosomes and lysosomes, resulting in inhibition of endosomal acidification and lysosomal enzyme activity. Because acidic pH of endosomes is a prerequisite of endosomal TLR activation, quinacrine can serve as an antagonist for endosomal TLRs. Quinacrine and its analog chloroquine are also known to act as therapeutic agents for autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus, of which therapeutic activity is due to suppression of TLR9 activity as shown by researchers.

Limitations

This product is for research use only and is not approved for use in humans or in clinical diagnosis. Inhibitors are guaranteed for 1 year from date of receipt.

Publications for Quinacrine Inhibitor (NBP2-29385)(1)

Publication using NBP2-29385

• Choudhuri S, Garg NJ PARP1-cGAS-NF-kappa B pathway of proinflammatory macrophage activation by extracellular vesicles released during Trypanosoma cruzi infection and Chagas disease PLoS Pathog. 2020-04-01 [PMID: 32315358]