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Chloroquine

Chloroquine

产品编号 T8689   CAS 54-05-7

Chloroquine 是一种 Toll 样受体抑制剂,可以抑制自噬。Chloroquine 具有抗疟疾和抗炎活性,广泛用于治疗疟疾和类风湿性关节炎。Chloroquine 还具有抗 SARS-CoV-2 (COVID-19) 活性、抗 HIV-1 活性。

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Chloroquine Chemical Structure
Chloroquine, CAS 54-05-7
规格 价格/CNY 货期 数量
100 mg ¥ 415 现货
200 mg ¥ 726 现货
500 mg ¥ 1,463 现货
1 mL * 10 mM (in DMSO) ¥ 208 现货
其他形式的 Chloroquine:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
产品目录号及名称: Chloroquine (T8689)
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纯度: 99.98%
纯度: 99.96%
纯度: 99.94%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
体外活性 方法:人胆管癌细胞 QBC939 用 Chloroquine (1.2-200 µM) 处理 24 h,使用 MTT 方法检测细胞生长抑制情况。
结果:Chloroquine 剂量依赖性地抑制 HRECs 细胞生长,IC50 为 53.01 µM。[1]
方法:人非小细胞肺癌细胞 A549 用 Chloroquine (10-80 μM) 处理 24 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Chloroquine 诱导 LC3-II 的表达增强,而 LC3-I 的表达降低,导致 LC3-II/LC3-I 比率增加,40 μM Chloroquine 处理时 LC3-II/LC3-I 的比率最高。[2]
方法:人骨肉瘤细胞 U2OS 和人宫颈癌细胞 HeLa 用 Chloroquine (100 μM) 处理 5 h,使用 Immunofluorescence 方法检测晚期内体区室和溶酶体的标志蛋白 LAMP1。
结果:Chloroquine 增加了 LAMP1 阳性结构的面积。[3]
体内活性 方法:为研究 Chloroquine 对急性肝损伤的作用及其潜在分子机制,在 CCl4 (10 mL/kg) 注射前 2-24 h,将 Chloroquine (5-50 mg/kg) 单剂量腹腔注射给 C57BL/6 小鼠。
结果:Chloroquine 预处理显著抑制了 CCl4 诱导的急性肝损伤,表现为血清转氨酶、天冬氨酸转氨酶降低和肝损伤组织学评分降低。Chloroquine 预处理下调 CCl4 诱导的肝组织高迁移率组蛋白1 (HMGB1) 的表达和血清 HMGB1 以及 IL-6 和 TNF-α 的水平。[4]
方法:为研究 Chloroquine 与视网膜病变的关系,将 Chloroquine (50 mg/kg ) 腹腔注射给 C57/BL6 小鼠,每周三次,持续六周。
结果: 长期使用 Chloroquine 诱发小鼠视网膜病变。Chloroquine 治疗的小鼠视网膜中炎症小体成分 IL-1β mRNA 和 caspase1 的 mRNA 增加,这与炎症小体的启动一致,NTPDase1 也增加,表明视网膜中细胞外ATP增加。[5]
化合物与蛋白结合的复合物

T8689_2

CHLOROQUINE BINDS IN THE COFACTOR BINDING SITE OF PLASMODIUM FALCIPARUM LACTATE DEHYDROGENASE.

分子量 319.87
分子式 C18H26ClN3
CAS No. 54-05-7

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (312.63 mM)

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

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 3.1263 mL 15.6314 mL 31.2627 mL 78.1568 mL
5 mM 0.6253 mL 3.1263 mL 6.2525 mL 15.6314 mL
10 mM 0.3126 mL 1.5631 mL 3.1263 mL 7.8157 mL
20 mM 0.1563 mL 0.7816 mL 1.5631 mL 3.9078 mL
50 mM 0.0625 mL 0.3126 mL 0.6253 mL 1.5631 mL
100 mM 0.0313 mL 0.1563 mL 0.3126 mL 0.7816 mL

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TargetMol Library Books参考文献

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.

TargetMol Library Books文献引用

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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Atazanavir sulfate CDD-1733 NSC89641 SARS-CoV-2-IN-39 CDD-1845 SARS-CoV-2 3CLpro-IN-19 PLpro inhibitor SARS-CoV-2-IN-60

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗寄生虫天然产物库 抗癌上市药物库 抗癌临床化合物库 药物功能重定位化合物库 抗寄生虫库 抗癌药物库 FDA 上市药物库 ReFRAME 相关化合物库 上市药物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

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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