Hydroxychloroquine Sulfate

Catalog No.S4430

Hydroxychloroquine Sulfate Chemical Structure

Molecular Weight(MW): 433.95

Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.

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  • (A) CNE-2 and HONE-1 cells were treated with lapatinib (0–10 μM) or DMSO control for 48 hours in the presence or absence of 20 μM of HCQ. At the end of treatment, cell viability was assessed by CCK-8 assay. Results are shown as the mean ± standard deviation. *P<0.05; **P<0.01. (B) CNE-2 and HONE-1 cells were treated with lapatinib (0–5 μM) or DMSO control for 48 hours. Phospho-eEF-2 and eEF-2 were examined by western blotting. GAPDH was used as a loading control.

    Onco Targets Ther, 2016, 9:6195-6201.. Hydroxychloroquine Sulfate purchased from Selleck.

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Biological Activity

Description Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Targets
TLR9 [5] Autophagy [1]
In vitro

Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis[2].

In vivo The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent[3]. In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals[4].

Protocol

Kinase Assay:[2]
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In vitro kinase assays:

with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.
Cell Research:[2]
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  • Cell lines: Human RCC cell lines
  • Concentrations: 75 or 100 μM
  • Incubation Time: 48 h
  • Method: All cells are cultured in RPMI with 10% FBS, 1% glutamine, and 1% Pen/Strep. cells are seeded on the appropriated plates overnight and treated with HCQ (75 or 100 μM) for 48 hours.
    (Only for Reference)

Solubility (25°C)

In vitro Water 67 mg/mL (154.39 mM)
DMSO <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.95
Formula

C18H28ClN3O5S

CAS No. 747-36-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02874287 Not yet recruiting Coronary Artery Disease First Affiliated Hospital Xian Jiaotong University August 2016 Phase 4
NCT02942381 Recruiting IgA Patients|Hydroxychloroquine Peking University First Hospital August 2016 Phase 2
NCT02765594 Recruiting Primary IgA Nephropathy Peking Union Medical College Hospital May 2016 Phase 4
NCT02615938 Recruiting Interstitial Lung Disease|Diffuse Parenchymal Lung Disease|Children´s Interstitial Lung Disease Matthias Griese|Ludwig-Maximilians - University of Munich April 2015 Phase 2
NCT02351752 Completed Primary IgA Nephropathy LLiu|Peking University First Hospital January 2015 Phase 4
NCT00946790 Completed Immunosuppression|Rheumatism Sandoz July 1993 Phase 1

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID