Hydroxychloroquine Sulfate

Catalog No.S4430 Synonyms: HCQ

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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4 Customer Reviews

  • C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).

    Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1489. Hydroxychloroquine Sulfate purchased from Selleck.

    Expression levels of LC3-I and LC3-II were analyzed by western blotting at 80 and 120 min following BBR-SDT with or without 3MA- and hydroxychloroquine-pretreatments. Quantification of the LC3-II/LC3-I ratios are shown (n=3; *Po0.05, **Po0.01, ***Po0.001 versus control, # P<0.05, ##P<0.01 versus BBR-SDT groups)

    Cell Death Dis, 2017, 8(1):e2558. Hydroxychloroquine Sulfate purchased from Selleck.

  • The effect of 3-MA, hydroxychloroquine, and ba A1 with or without HSYA-SDT on the expression levels of the autophagy-related proteins p62 and LC3 and quantifications of the LC3-ΙΙ/LC3-Ι ratio and p62 are shown. All data are mean ± standard error (n=5). ∗

    Oxid Med Cell Longev, 2017, 8519169. Hydroxychloroquine Sulfate purchased from Selleck.

    (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 Insoluble
Ethanol 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 HCQ

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03592823 Recruiting Atrial Fibrillation First Affiliated Hospital of Harbin Medical University August 1 2018 Phase 4
NCT02874287 Recruiting Coronary Artery Disease First Affiliated Hospital Xi''an Jiaotong University October 8 2017 Phase 4
NCT02942381 Completed IgA Patients|Hydroxychloroquine Peking University First Hospital September 13 2016 Phase 2
NCT02765594 Recruiting Primary IgA Nephropathy Peking Union Medical College Hospital June 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

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID