Hydroxychloroquine sulfate

Biological Activity

Hydroxychloroquine sulfate is an autophagy inhibitor. Also inhibits TLR9. Inhibits growth and induces apoptosis of renal cancer cells in vitro. Additionally inhibits PRC2 by inhibiting the allosteric binding of PRC2 to EED (embryonic ectoderm development) within the H3K27me3-binding pocket, and reduces H3K27me3 levels in multiple myeloma cells in vitro. Inhibits SARS-CoV-2 viral infection, in vitro (EC₅₀ values in μM range and dependent on viral RNA copy number). Hydroxychloroquine improves efficacy of adeno-associated viral gene transduction in vivo and in vitro. Also antimalarial and immunomodulator.

Tocris products are for biomedical research use only. They are not intended for human or veterinary use.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Hydroxychloroquine Destabilizes Phospho-S6 in Human Renal Carcinoma Cells.
   Lee HO, Mustafa A, Hudes GR, Kruger WD.
   PLoS One.
2. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo.
   Lamphier et al.
   Mol.Pharmacol., 2014;85:429
3. A drug repurposing screening reveals a novel epigenetic activity of hydroxychloroquine.
   Catalano et al.
   Eur.J.Med.Chem., 2019;183
4. Hydroxychloroquine, a less toxic derivative of chloroquine, is effective in inhibiting SARS-CoV-2 infection in vitro.
   Liu et al.
   Cell Discovery, 2020;6:16

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