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Chloroquine

Catalog No. T8689   CAS 54-05-7

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

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Chloroquine Chemical Structure
Chloroquine, CAS 54-05-7
Pack Size Availability Price/USD Quantity
100 mg In stock $ 54.00
200 mg In stock $ 94.00
500 mg In stock $ 189.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.98%
Purity: 99.96%
Purity: 99.94%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
In vitro METHODS: Human cholangiocarcinoma cells QBC939 were treated with Chloroquine (1.2-200 µM) for 24 h. Cell growth inhibition was detected by MTT.
RESULTS: Chloroquine dose-dependently inhibited the cell growth of HRECs with an IC50 of 53.01 µM. [1]
METHODS: Human non-small cell lung cancer cells A549 were treated with Chloroquine (10-80 μM) for 24 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: Chloroquine induced an increase in LC3-II expression and a decrease in LC3-I expression, resulting in an increase in the LC3-II/LC3-I ratio. The highest LC3-II/LC3-I ratio was observed with 40 μM Chloroquine treatment. [2]
METHODS: Human osteosarcoma cells U2OS and human cervical cancer cells HeLa were treated with Chloroquine (100 μM) for 5 h. LAMP1, a marker protein for late endosomal compartment and lysosome, was detected by Immunofluorescence.
RESULTS: Chloroquine increased the area of LAMP1 positive structures. [3]
In vivo METHODS: To investigate the effects of Chloroquine on acute liver injury and its potential molecular mechanisms, a single dose of Chloroquine (5-50 mg/kg) was administered intraperitoneally to C57BL/6 mice 2-24 h before CCl4 (10 mL/kg) injection.
RESULTS: Chloroquine pretreatment significantly inhibited CCl4-induced acute liver injury, as evidenced by a decrease in serum aminotransferases, aspartate aminotransferase, and a decrease in the histological score of liver injury, and down-regulated CCl4-induced high-mobility histone 1 (HMGB1) expression in liver tissues as well as the levels of serum HMGB1, IL-6, and TNF-α. levels. [4]
METHODS: To investigate the relationship between Chloroquine and retinopathy, Chloroquine (50 mg/kg ) was administered intraperitoneally to C57/BL6 mice three times a week for six weeks.
RESULTS: Chronic administration of Chloroquine induced retinopathy in mice. mRNAs for IL-1β mRNA, a component of inflammatory vesicles, and caspase1 were increased in the retinas of Chloroquine-treated mice, consistent with the initiation of inflammatory vesicles, and NTPDase1 was increased, suggesting an increase in extracellular ATP in the retina. [5]
Molecular Weight 319.87
Formula C18H26ClN3
CAS No. 54-05-7

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (312.63 mM)

Ethanol: 100 mg/mL (312.63 mM), sonification is recommended.

TargetMolReferences and Literature

1. Jia B, et al. Autophagy inhibitor chloroquine induces apoptosis of cholangiocarcinoma cells via endoplasmic reticulum stress. Oncol Lett. 2018 Sep;16(3):3509-3516. 2. Liu L, et al. Chloroquine inhibits cell growth in human A549 lung cancer cells by blocking autophagy and inducing mitochondrial‑mediated apoptosis. Oncol Rep. 2018 Jun;39(6):2807-2816. 3. Mauthe M, et al. Chloroquine inhibits autophagic flux by decreasing autophagosome-lysosome fusion. Autophagy. 2018;14(8):1435-1455. 4. Dai C, et al. Chloroquine ameliorates carbon tetrachloride-induced acute liver injury in mice via the concomitant inhibition of inflammation and induction of apoptosis. Cell Death Dis. 2018 Nov 26;9(12):1164. 5. Wennan L, et al. Increased inflammasome priming and microglial activation in a mouse model of chloroquine retinopathy. Investigative Ophthalmology & Visual Science. 2016 September; 57:2237. 6. Chen J, Li J, Chen J, et al. Treatment of collagen-induced arthritis rat model by using Notch signalling inhibitor[J]. Journal of Orthopaedic Translation. 2021, 28: 100-107. 7. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1[J]. Frontiers in Pharmacology. 2021, 11: 2233. 8. Wang M, Xu Y, Zhang Y, et al. Deciphering the autophagy regulatory network via single-cell transcriptome analysis reveals a requirement for autophagy homeostasis in spermatogenesis[J]. Theranostic. 2021, 11(10): 5010.

TargetMolCitations

1. Yan C, Zheng L, Jiang S, et al.Exhaustion-associated cholesterol deficiency dampens the cytotoxic arm of antitumor immunity.Cancer Cell.2023 2. Ding L, Chen X, Zhang W, et al.Canagliflozin primes antitumor immunity by triggering PD-L1 degradation in endocytic recycling.The Journal of Clinical Investigation.2023, 133(1). 3. Yu Q, Li C, Niu Q, et al.Hepatic COX1 loss leads to impaired autophagic flux and exacerbates nonalcoholic steatohepatitis.Acta Pharmaceutica Sinica B.2023 4. Zhang W, Pan X, Xu Y, et al.Mevalonate improves anti-PD-1/PD-L1 efficacy by stabilizing CD274 mRNA.Acta Pharmaceutica Sinica B.2023 5. Liu X, Fang Y, Lv X, et al.Deubiquitinase OTUD6A in macrophages promotes intestinal inflammation and colitis via deubiquitination of NLRP3.Cell Death & Differentiation.2023: 1-15. 6. Lei S, Chen C, Han F, et al.AMER1 deficiency promotes the distant metastasis of colorectal cancer by inhibiting SLC7A11-and FTL-mediated ferroptosis.Cell Reports.2023, 42(9). 7. Xiang H, Liu R, Zhang X, et al.Discovery of Small-Molecule Autophagy Inhibitors by Disrupting the Protein–Protein Interactions Involving Autophagy-Related 5.Journal of Medicinal Chemistry.2023 8. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 9. Zhao L, Zhang W, Luan F, et al.Butein suppresses PD-L1 expression via downregulating STAT1 in non-small cell lung cancer.Biomedicine & Pharmacotherapy.2023, 157: 114030. 10. Zhang M, Jia X, Cheng C, et al.Capsaicin functions as a selective degrader of STAT3 to enhance host resistance to viral infection.Acta Pharmacologica Sinica.2023: 1-12.
11. Han S, Zhang H, Liu X, et al.Enhanced autophagy reversed aflatoxin B1-induced decrease in lactate secretion of dairy goat Sertoli cells.Ecotoxicology and Environmental Safety.2023, 259: 115063. 12. Jiao J, Ruan L, Cheng C, et al.Paired protein kinases PRKCI-RIPK2 promote pancreatic cancer growth and metastasis via enhancing NF-κB/JNK/ERK phosphorylation.Molecular Medicine.2023, 29(1): 1-17. 13. Shan X, Jiang R, Gou D, et al.Identification of a diketopiperazine‐based O‐GlcNAc transferase inhibitor sensitizing hepatocellular carcinoma to CDK9 inhibition.The FEBS Journal.2023 14. Cao P, Wang Y, Zhang C, et al.Quercetin ameliorates non-alcoholic fatty liver disease (NAFLD) via the promotion of AMPK-mediated hepatic mitophagy.The Journal of Nutritional Biochemistry.2023: 109414. 15. Xiang H, Wang R.Discovery of small-molecule inhibitors for the protein-protein interactions involving ATG5.Autophagy Reports.2023, 2(1): 2215617. 16. Zhou Y, Li Q, Zheng J, et al. N-Glycosylation on Asn50 of SND1 Is Required for Glioma U87 Cell Proliferation and Metastasis. Journal of Immunology Research. 2022 17. Wang J, Su Q, Wu Q, et al. Sanguinarine impairs lysosomal function and induces ROS-dependent mitophagy and apoptosis in human hepatocellular carcinoma cells. Archives of Pharmacal Research. 2021: 1-12. 18. Su G, Yang W, Wang S, et al. SIRT1-autophagy axis inhibits excess iron-induced ferroptosis of foam cells and subsequently increases IL-1Β and IL-18. Biochemical and Biophysical Research Communications. 2021, 561: 33-39. 19. Xiao Q, Lei L, Ren J, et al. Mutant NPM1-Regulated FTO-Mediated m6A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Frontiers in Oncology. 2022.12 20. Wang M, Xu Y, Zhang Y, et al. Deciphering the autophagy regulatory network via single-cell transcriptome analysis reveals a requirement for autophagy homeostasis in spermatogenesis. Theranostic. 2021 Mar 5;11(10):5010-5027. doi: 10.7150/thno.55645. eCollection 2021. 21. Nicholson M W, Huang C Y, Wang J Y, et al. Cardio-and Neurotoxicity of Selected Anti-COVID-19 Drugs. Pharmaceuticals. 2022, 15(6): 765 22. Wang F, Xie M, Chen P, et al. Homoharringtonine combined with cladribine and aclarubicin (HCA) in acute myeloid leukemia: A new regimen of conventional drugs and its mechanism. Oxidative Medicine and Cellular Longevity. 2022 23. Chen J, Li J, Chen J, et al. Treatment of collagen-induced arthritis rat model by using Notch signalling inhibitor. Journal of Orthopaedic Translation. 2021, 28: 100-107. 24. Pan X, Li R, Guo H, et al. Dihydropyridine Calcium Channel Blockers Suppress the Transcription of PD-L1 by Inhibiting the Activation of STAT1. Frontiers in Pharmacology. 2021 Jan 13;11:539261. doi: 10.3389/fphar.2020.539261. eCollection 2020. 25. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization. Reproduction. 2021, 1(aop). 26. Dai H, Wang J, Huang Z, et al. LncRNA OIP5-AS1 Promotes the Autophagy-Related Imatinib Resistance in Chronic Myeloid Leukemia Cells by Regulating miR-30e-5p/ATG12 Axis. Technology in cancer research & treatment. 2021, 20: 15330338211052150. 27. Wang W, Li S, Xu X, et al. Danshensu alleviates pseudo-typed SARS-CoV-2 induced mouse acute lung inflammation. Acta Pharmacologica Sinica. 2021: 1-10. 28. Su C, Cheng C, Rong Z, et al.Repurposing fluphenazine as an autophagy modulator for treating liver cancer.Heliyon.2023 29. Zhang M, Tan H, Gong Y, et al.TRIM26 restricts Epstein–Barr virus infection in nasopharyngeal epithelial cells through K48‐linked ubiquitination of HSP‐90β.The FASEB Journal.2024, 38(1): e23345. 30. Cui H, Zhu B, Li H, et al.Malonate differentially affects cell survival and confers chemoresistance in cancer cells via the induction of p53-dependent autophagy.Biochemical Pharmacology.2023: 115950. 31. Han Y, Wang C, Lu K, et al.Bovine parainfluenza type 3 virus induces incomplete autophagy to promote viral replication by activated beclin1 in vitro.Veterinary Microbiology.2024: 109972. 32. Chen H, Hu J, Xiong X, et al.AURKA inhibition induces Ewing’s sarcoma apoptosis and ferroptosis through NPM1/YAP1 axis.Cell Death & Disease.2024, 15(1): 99. 33. Liu T, Yue X, Chen X, et al.Nilotinib in combination with sunitinib renders MCL-1 for degradation and activates autophagy that overcomes sunitinib resistance in renal cell carcinoma.Cellular Oncology.2024: 1-18. 34. Ren Y L, Jiang Z, Wang J Y, et al.Loss of CHCHD2 Stability Coordinates with C1QBP/CHCHD2/CHCHD10 Complex Impairment to Mediate PD-Linked Mitochondrial Dysfunction.Molecular Neurobiology.2024: 1-21. 35. Li L, Fu S, Wang J, et al.SRT1720 inhibits bladder cancer cell progression by impairing autophagic flux.Biochemical Pharmacology.2024: 116111. 36. Hou G, Hu W, Sang Y, et al.Corynoxine triggers cell death via activating PP2A and regulating AKT-mTOR/GSK3β axes in NSCLC.Biochemical Pharmacology.2024: 116110.
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Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Antiparasitic Natural Product Library Anti-Cancer Approved Drug Library Anti-Parasitic Compound Library Anti-Infection Compound Library Antibiotics Library Autophagy Compound Library Selected Plant-Sourced Compound Library Drug Repurposing Compound Library

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Keywords

Chloroquine 54-05-7 Autophagy Immunology/Inflammation Microbiology/Virology Proteases/Proteasome SARS-CoV TLR HIV Protease Antibiotic Parasite Inhibitor SARS coronavirus malaria rheumatoid COVID-19 Toll-like Receptor (TLR) immune-modulating arthritis Human immunodeficiency virus HIV inflammatory inhibit infection inhibitor

 

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