Hydroxychloroquine (HCQ) Sulfate

Catalog No.S4430 Batch:S443010

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Technical Data

Formula

C18H28ClN3O5S
Molecular Weight 433.95 CAS No. 747-36-4
Solubility (25°C)* In vitro Water 87 mg/mL (200.48 mM)
DMSO Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Hydroxychloroquine (HCQ) 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 (from reference)

Kinase Assay:

[2]
  • 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 Assay:

[2]
  • 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.

Customer Product Validation

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1489]

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):272]

Data from [Data independently produced by , , Cell Death Dis, 2017, 8(1):e2558]

Data from [Data independently produced by , , Oxid Med Cell Longev, 2017, 8519169]

Selleck's Hydroxychloroquine (HCQ) Sulfate has been cited by 108 publications

Acetylation of MOB1 mediates polyphyllin II-reduced lysosome biogenesis in breast cancer by promoting the cytoplasmic retention of the YAP/TFEB coactivator complex [ Phytomedicine, 2024, 10.1016/j.phymed.2023.155152] PubMed: 37922793
Small molecule inhibitor targeting the Hsp70-Bim protein-protein interaction in estrogen receptor-positive breast cancer overcomes tamoxifen resistance [ Breast Cancer Res, 2024, 26(1):33] PubMed: 38409088
ATG7/GAPLINC/IRF3 axis plays a critical role in regulating pathogenesis of influenza A virus [ PLoS Pathog, 2024, 20(1):e1011958] PubMed: 38227600
The nucleotide-sensing Toll-Like Receptor 9/Toll-Like Receptor 7 system is a potential therapeutic target for IgA nephropathy [ Kidney Int, 2023, 104(5):943-955] PubMed: 37648155
Single-cell sequencing of ascites fluid illustrates heterogeneity and therapy-induced evolution during gastric cancer peritoneal metastasis [ Nat Commun, 2023, 14(1):822] PubMed: 36788228
AR antagonists develop drug resistance through TOMM20 autophagic degradation-promoted transformation to neuroendocrine prostate cancer [ J Exp Clin Cancer Res, 2023, 42(1):204] PubMed: 37563661
Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer [ Cancer Res, 2023, 83(1):141-157] PubMed: 36346366
Tetrandrine synergizes with MAPK inhibitors in treating KRAS-mutant pancreatic ductal adenocarcinoma via collaboratively modulating the TRAIL-death receptor axis [ Pharmacol Res, 2023, 197:106955] PubMed: 37820855
Platelet factor 4 limits neutrophil extracellular trap- and cell-free DNA-induced thrombogenicity and endothelial injury [ JCI Insight, 2023, 8(22)e171054] PubMed: 37991024
PSGL-1 is an evolutionarily conserved antiviral restriction factor [ mBio, 2023, 10.1128/mbio.00387-23] PubMed: 37787515

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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