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Submit ReviewHydroxychloroquine 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.
M. Wt | 433.95 |
Formula | C18H28ClN3O5S |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 747-36-4 |
PubChem ID | 12947 |
InChI Key | JCBIVZZPXRZKTI-UHFFFAOYSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 43.4 | 100 |
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.
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 |
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.
Keywords: Hydroxychloroquine sulfate, Hydroxychloroquine sulfate supplier, TLR9, toll-like, receptors, inhibitors, autophagy, inhibits, cancer, immunomodulator, antimalarial, PRC2, polycomb, repressive, complex, EED, aav, viral, gene, transduction, transducer, adeno-associated, virus, Toll-like, Receptors, Autophagy, Other, Lysine, Methyltransferases, COVID-19, Endocytosis, Antimalarials, Coronavirus, Viral, Transduction, Enhancers, 5648, Tocris Bioscience
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Combinatorial treatments of hydroxychloroquine sulfate with chemotherapeutics led to synergistic apoptotic phenotype in vitro.
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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.