Hydroxychloroquine (HCQ) Sulfate

Catalog No.S4430 Batch:S443006

Print

Technical Data

Formula

C18H28ClN3O5S
Molecular Weight 433.95 CAS No. 747-36-4
Solubility (25°C)* In vitro Water 86 mg/mL (198.17 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.)

Preparing Stock Solutions

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.

References

  • https://pubmed.ncbi.nlm.nih.gov/19357706/
  • https://pubmed.ncbi.nlm.nih.gov/26134285/
  • https://pubmed.ncbi.nlm.nih.gov/26636577/
  • http://acrabstracts.org/abstract/effects-of-in-vivo-treatment-with-hydroxychloroquine-on-endothelial-function-in-a-murine-model-of-systemic-lupus-erythematosus/
  • https://pubmed.ncbi.nlm.nih.gov/24342772/

Customer Product Validation

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).

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

Expression levels of proteins involved in autophagy and apoptosis signaling in GC (gastric cancer) cells after treatments for 48 h. The treatments were the same as those in 5c. All proteins were normalized to β-actin

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

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)

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

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). ∗

Data from [ , , Oxid Med Cell Longev, 2017, 8519169 ]

Selleck's Hydroxychloroquine (HCQ) Sulfate Has Been Cited by 126 Publications

BMAL1-depletion remodels ceramide metabolism to regulate ferroptosis and sorafenib chemosensitivity in acute myeloid leukemia [ iScience, 2025, 28(4):112054] PubMed: 40241743
MYC Overexpression Enhances Sensitivity to MEK Inhibition in Head and Neck Squamous Cell Carcinoma [ Int J Mol Sci, 2025, 26(2)588] PubMed: 39859304
Gossypin induces apoptosis and autophagy via the MAPK/JNK pathway in HT‑29 human colorectal cancer cells [ Int J Mol Med, 2025, 56(1)107] PubMed: 40376978
Glycopolymer nanomicelles: pH-responsive drug delivery, endocytosis pathway, autophagy behavior, and the effect of autophagy inhibitors [ J Mater Sci-Mater M, 2025, 36(1):47] PubMed: 40478478
TRIM22 inhibits the metastasis of colorectal cancer through facilitating β-Catenin degradation [ Exp Cell Res, 2025, 446(2):114473] PubMed: 39978715
Pyrimethamine Inhibits Human Ovarian Cancer by Triggering Lethal Mitophagy via Activating the p38/JNK/ERK Pathway [ Oncol Res, 2025, 33(9):2421-2434] PubMed: 40918465
Itaconate drives pro-inflammatory responses through proteasomal degradation of GLO1 [ Biochem Biophys Res Commun, 2025, 747:151292] PubMed: 39787788
Platelet factor 4 modulates endothelial cell antimicrobial activity to enhance bacterial clearance and improve sepsis outcomes [ bioRxiv, 2025, 2025.09.02.673783] PubMed: 40950105
Inhibition of ethanol-induced eNAMPT secretion attenuates liver ferroptosis through BAT-Liver communication [ Redox Biol, 2024, 75:103274] PubMed: 39059204
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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.