Chloroquine phosphate

产品编号: T0194 别名:

Chloroquine diphosphate,磷酸氯喹,Chingamin phosphate,Aralen phosphate

Chloroquine diphosphate 是广泛用于疟疾和类风湿性关节炎的抗疟疾和抗炎剂。它是Autophagy和toll-like receptors 抑制剂，有效抑制SARS-CoV-2(COVID-19) 感染 (EC50=1.13 μM)。

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Chloroquine phosphate Chemical Structure

CAS：50-63-5

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

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

体外活性

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].

体内活性

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].

细胞实验

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].

动物实验

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].

Cas No.

50-63-5

分子式

C18H32ClN3O8P2

分子量

515.86

别名

Chloroquine diphosphate;磷酸氯喹;Chingamin phosphate;Aralen phosphate;Chloroquine phosphate

参考文献

[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]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 [3]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.[4]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.[5]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.[6]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.[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.

引用文献

[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

储存和溶解度

DMSO:Insoluble
H2O:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Chloroquine phosphate 50-63-5

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Keywords

inhibit Chloroquine diphosphate COVID-19 Chloroquine phosphate Autophagy Chloroquine Inhibitor rheumatoid immune-modulating Toll-like Receptor (TLR) Antibiotic HIV SARS coronavirus infection Parasite 磷酸氯喹 Human immunodeficiency virus arthritis malaria inflammatory Chingamin phosphate Aralen phosphate SARS-CoV 50-63-5

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Chloroquine phosphate

Chloroquine diphosphate,磷酸氯喹,Chingamin phosphate,Aralen phosphate

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