Hydroxychloroquine (HCQ), Autophagy and TLR9 Inhibitor

Hydroxychloroquine (HCQ) is a potent autophagy inhibitor and TLR9 inhibitor. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process. In cancer cells, HCQ treatment has been shown to cause increased apoptosis, tumor regression, and delay in tumor recurrence. HCQ was an effective growth inhibitor of human RCC cell lines, inhibiting growth, promoting apoptosis, and effecting cellular metabolism. HCQ altered the levels of the mTORC1 activation marker phospho-S6 and that this effect was mediated by a different mechanism than that observed for the mTOR inhibitor RAD001. HCQ is also a potent inhibitor of TLR9, prevents DNA-TLR9 interaction in vitro and modulates signaling in vivo.

Product information

CAS Number: 747-36-4

Molecular Weight: 433.95

Formula: C18H28ClN3O5S

Chemical Name: 2-((4-((7-chloroquinolin-4-yl)amino)pentyl)(ethyl)amino)ethan-1-ol sulfate

Smiles: CCN(CCO)CCCC(C)NC1=CC=NC2=CC(Cl)=CC=C21.OS(O)(=O)=O

InChiKey: JCBIVZZPXRZKTI-UHFFFAOYSA-N

InChi: InChI=1S/C18H26ClN3O.H2O4S/c1-3-22(11-12-23)10-4-5-14(2)21-17-8-9-20-18-13-15(19)6-7-16(17)18;1-5(2,3)4/h6-9,13-14,23H,3-5,10-12H2,1-2H3,(H,20,21);(H2,1,2,3,4)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Hydroxychloroquine (HCQ) was used at 50-100 µM final concentration in various assays.

In Vivo:

Hydroxychloroquine (HCQ) can be dosed to mice orally at 50 mg/Kg once per day.

References:

1. Lee HO, et al. Hydroxychloroquine Destabilizes Phospho-S6 in Human Renal Carcinoma Cells. (2015) PLoS One. 10(7):e0131464.
2. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. (2014) Mol Pharmacol. 85(3):429-40.

Products are for research use only. Not for human use.

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