Hydroxychloroquine sulfate

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Description: Autophagy inhibitor; also TLR9 inhibitor
Chemical Name: 2-[[4-[(7-Chloro-4-quinolinyl)amino]pentyl]ethylamino]ethanol sulfate
Purity: ≥99% (HPLC)
Reviews (1)
Literature (3)

Biological Activity for Hydroxychloroquine sulfate

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 for Hydroxychloroquine sulfate

M. Wt 433.95
Formula C18H28ClN3O5S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 747-36-4
PubChem ID 12947
Smiles ClC(C=C1)=CC2=C1C(NC(CCCN(CC)CCO)C)=CC=N2.OS(=O)(O)=O

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.

Solubility Data for Hydroxychloroquine sulfate

Solvent Max Conc. mg/mL Max Conc. mM
water 43.4 100

Preparing Stock Solutions for Hydroxychloroquine sulfate

The following data is based on the product molecular weight 433.95. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.3 mL 11.52 mL 23.04 mL
5 mM 0.46 mL 2.3 mL 4.61 mL
10 mM 0.23 mL 1.15 mL 2.3 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets for Hydroxychloroquine sulfate

Certificate of Analysis / Product Datasheet
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References for Hydroxychloroquine sulfate

References are publications that support the biological activity of the product.

Lee et al (2015) Hydroxychloroquine Destabilizes Phospho-S6 in Human Renal Carcinoma Cells. PLoS ONE 10 e0131464 PMID: 26134285

Lamphier et al (2014) Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol.Pharmacol. 85 429 PMID: 24342772

Catalano et al (2019) A drug repurposing screening reveals a novel epigenetic activity of hydroxychloroquine. Eur.J.Med.Chem. 183 PMID: 31550663

Liu et al (2020) Hydroxychloroquine, a less toxic derivative of chloroquine, is effective in inhibiting SARS-CoV-2 infection in vitro. Cell Discovery 6 16 PMID: 32194981

Chandler et al (2019) Enhancement of adeno-associated virus-mediated gene therapy using hydroxychloroquine in murine and human tissues. Mol.Ther.Methods Clin.Dev. 14 77 PMID: 31309129

If you know of a relevant reference for Hydroxychloroquine sulfate, please let us know.

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Citations for Hydroxychloroquine sulfate

Citations are publications that use Tocris products.

Currently there are no citations for Hydroxychloroquine sulfate. Do you know of a great paper that uses Hydroxychloroquine sulfate from Tocris? Please let us know.

Reviews for Hydroxychloroquine sulfate

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Apoptosis induction.
Assay Type: In Vitro
Species: Human

Combinatorial treatments of hydroxychloroquine sulfate with chemotherapeutics led to synergistic apoptotic phenotype in vitro.

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Autophagy Scientific Review

Autophagy Scientific Review

Written by Patricia Boya and Patrice Codogno, this review summarizes the molecular mechanisms, physiology and pathology of autophagy. The role of autophagy in cell death and its links to disease are also discussed. Compounds available from Tocris are listed.

Autophagy Poster

Autophagy Poster

Autophagy is a cellular process used by cells for degradation and recycling. Written by Patricia Boya and Patrice Codogno, this poster summarizes the molecular machinery, physiology and pathology of autophagy. Compounds available from Tocris are listed.

Programmed Cell Death Poster

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.