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Chloroquine phosphate

Catalog No. T0194 CAS 50-63-5

Synonyms: Chloroquine diphosphate, Chingamin phosphate, Aralen phosphate

Chloroquine is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

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Chloroquine phosphate, CAS 50-63-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Chloroquine is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).
Targets&IC50	Cytotoxicity against human K562 cells by MTT assay:31.83 nM, Cytotoxicity against hμMan KB cells by microplate method:0.6 μM
In vitro	Chloroquine (20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells [1]. Chloroquine (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine has cell-, dose- and hypoxia-dependent effects on MMP-2, MMP-9 and MMP-13 mRNA expression [2]. TLR7 and TLR9 inhibition using chloroquine significantly reduce HuH7 cell proliferation in vitro [3].
In vivo	Chloroquine (80 mg/kg, i.p.) does not prevent the growth of the triple-negative MDA-MB-231 cells with high or low TLR9 expression levels in the orthotopic mouse model [2]. TLR7 and TLR9 inhibition using chloroquine significantly inhibit tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine [3].
Cell Research	The cells are cultured in 6-well plates with normal culture medium in the presence of vehicle or 25 or 50 μM chloroquine, until near confluency, after which they are rinsed with sterile phosphate-buffered saline (PBS) and cultured further for the indicated times in serum-free culture medium. At the desired time-points, the culture medium is discarded and the cells are quickly harvested in lysis buffer and clarified by centrifugation. Subsequent to boiling the supernatants in reducing sodium dodecyl sulfate (SDS) sample buffer, equal amounts of protein (100 μg) are loaded per lane and the samples are electrophoresed into 10 or 4-20% gradient polyacrylamide SDS gels, then transferred to a nitrocellulose membrane. To detect TLR9, the blots were incubated overnight at 4°C with anti-TLR9 antibodies, diluted 1:500 in Tris-buffered saline with 0.1% (v/v) Tween-20 (TBST). Equal loading is confirmed with polyclonal rabbit anti-actin. Secondary detection is performed with horseradish peroxidase-linked secondary antibodies. The protein bands are visualized by chemiluminescence using an ECL kit [2].
Animal Research	Control and TLR9 siRNA MDA-MB-231 cells (5×105 cells in 100 μL) are inoculated into the mammary fat pads of four-week-old, immune-deficient mice (athymic nude/nu Foxn1). Treatments are started seven days after tumor cell inoculation. The mice are treated daily either with intraperitoneal (i.p.) chloroquine (80 mg/kg) or vehicle (PBS). The animals are monitored daily for clinical signs. Tumor measurements are performed twice a week and tumor volume is calculated according to the formula V=(π/6) (d1×d2)3/2, where d1 and d2 are perpendicular tumor diameters. The tumors are allowed to grow for 22 days, at which point the mice are sacrificed and the tumors are dissected for a final measurement. Throughout the experiments, the animals are maintained under controlled pathogen-free environmental conditions (20-21°C, 30-60% relative humidity and a 12-h lighting cycle). The mice are fed with small-animal food pellets and supplied with sterile water ad libitum [2].

Synonyms	Chloroquine diphosphate, Chingamin phosphate, Aralen phosphate
Molecular Weight	515.87
Formula	C18H26CLN3·2(H3PO4)
CAS No.	50-63-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: Insoluble

H2O: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Said A, et al. Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells. J Immunol. 2014 Dec 15;193(12):6135-43. 2. Tuomela J, et al. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672. 3. Mohamed FE, et al. Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2014 Jul 2. doi: 10.1111/liv.12626. 4. Su Q, Wang J, Liu F, et al. Blocking Parkin/PINK1-mediated mitophagy sensitizes hepatocellular carcinoma cells to sanguinarine-induced mitochondrial apoptosis[J]. Toxicology in Vitro. 2020: 104840. 6. Hanyu X, Lanyue L, Miao D, et al. Effect of Ganoderma applanatum polysaccharides on MAPK/ERK pathway affecting autophagy in breast cancer MCF-7 cells[J]. International Journal of Biological Macromolecules. 2020, 146: 353-362 7. Zhou Y, Wang Y, Wu S, et al. Sulforaphane-cysteine inhibited migration and invasion via enhancing mitophagosome fusion to lysosome in human glioblastoma cells[J]. Cell Death & Disease. 2020, 11(9): 1-16. 8. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530.

Citations

1. Fu R, Yang P, Li Z, et al. Avenanthramide A triggers potent ROS-mediated anti-tumor effects in colorectal cancer by directly targeting DDX3. Cell Death & Disease. 2019, 10(8): 1-14 2. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 3. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 4. Zhou Y, Wang Y, Wu S, et al. Sulforaphane-cysteine inhibited migration and invasion via enhancing mitophagosome fusion to lysosome in human glioblastoma cells. Cell Death & Disease. 2020, 11(9): 1-16. 5. Hanyu X, Lanyue L, Miao D, et al. Effect of Ganoderma applanatum polysaccharides on MAPK/ERK pathway affecting autophagy in breast cancer MCF-7 cells. International Journal of Biological Macromolecules. 2020, 146: 353-362 6. Wang Y, Ji L, Peng Z, et al. Silencing DAPK3 blocks the autophagosome-lysosome fusion by mediating SNAP29 in trophoblast cells under high glucose treatment. Molecular and Cellular Endocrinology. 2020, 502: 110674 7. Su Q, Wang J, Liu F, et al. Blocking Parkin/PINK1-mediated mitophagy sensitizes hepatocellular carcinoma cells to sanguinarine-induced mitochondrial apoptosis. Toxicology in Vitro. 2020: 104840 8. Xi H, Hu Z, Han S, et al. FSH-inhibited autophagy protects against oxidative stress in goat Sertoli cells through p62-Nrf2 pathway. Theriogenology. 2022 9. Su Q, Wu Q, Chen K, et al. Induction of Estrogen Receptor β-mediated Autophagy Sensitizes Breast Cancer Cells to TAD1822-7, a Novel Biphenyl Urea Taspine Derivative. Molecular Biology Reports. 2021

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Keywords

Chloroquine phosphate 50-63-5 Autophagy Immunology/Inflammation Microbiology/Virology Proteases/Proteasome Parasite SARS-CoV TLR HIV Protease Antibiotic inhibit Chloroquine diphosphate COVID-19 Chloroquine Inhibitor rheumatoid immune-modulating Toll-like Receptor (TLR) HIV SARS coronavirus infection Human immunodeficiency virus arthritis malaria inflammatory Chingamin phosphate Aralen phosphate inhibitor

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