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Chloroquine/氯喹 {[allProObj[0].p_purity_real_show]}

貨號：A136097 同義名： NSC-187208; CHQ

Chloroquine 是一種抗瘧藥物，同時也是自噬抑制劑，對自噬過程具有抑制作用，IC50 值為 2.1 μM。Chloroquine 具有抗瘧、抗炎和抗腫瘤作用，可用于自噬研究和抗瘧疾治療。

Chloroquine/氯喹 化學結構 CAS號：54-05-7
Chloroquine/氯喹 化學結構
CAS號：54-05-7
Chloroquine/氯喹 3D分子結構
CAS號：54-05-7
Chloroquine/氯喹 化學結構 CAS號：54-05-7
Chloroquine/氯喹 3D分子結構 CAS號：54-05-7
規格 價格 會員價 庫存 數量
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Chloroquine/氯喹 純度/質量文件 產品僅供科研

貨號：A136097 標準純度： {[allProObj[0].p_purity_real_show]}
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產品名稱 HIV Protease ↓ HIV-1 caspid ↓ 其他靶點 純度
Dextran sulfate sodium salt(MW 40000) ? M.W 40000
Vicriviroc maleate ? 98%
Rosamultin ? 97%
Darunavir ? 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

 		99+%
Chloroquine ? Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

 		PXR 99%+
NBD-556 ? 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

 		99%+
Atazanavir Sulfate ? 98%
Limonin ? 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

 		98%
Ritonavir ? 98%
Azvudine ? 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

 		97%
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多，抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用，但抑制強度暫時沒有相關數據。
產品名稱 ATM ↓ ATR ↓ 其他靶點 純度
Wortmannin ++

ATM, IC50: 150 nM

 		MLCK,PI3K,DNA-PK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ? 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 98%
m-PEG25-NHS ester ++++

ATR, IC50: 7 nM

 		95%
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多，抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用，但抑制強度暫時沒有相關數據。
產品名稱 Autophagy ↓ 其他靶點 純度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

 		95%
Hydroxychloroquine sulfate ? 99%
Valproic acid sodium ? HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

 		99%+
ROC-325 ? 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		99%
Lys05 ? 99%+
1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多，抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用，但抑制強度暫時沒有相關數據。

Chloroquine/氯喹 生物活性

靶點

  • HIV Protease
描述 Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine (CHQ, 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 suppressed matrix metalloproteinase (MMP)-2 and MMP-9 mRNA expression and protein activity, whereas MMP-13 mRNA expression and proteolytic activity were increased. Despite enhancing TLR9 mRNA expression, chloroquine suppressed TLR9 protein expression in vitro. Daily treatment of mice with intraperitoneal (i.p.) chloroquine (80 mg/kg/day) for 22 days, did not inhibit the growth of control siRNA or TLR9 siRNA MDA-MB-231 breast cancer cells[2]. The combination of chloroquine with zinc enhanced chloroquine's cytotoxicity and induced apoptosis in A2780 cells[3]. Chloroquine (0.01-100μM; 48?hours) potently blocked virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC50=1.13?μM). Chloroquine blocks virus infection by increasing endosomal pH required for virus/cell fusion, as well as interfering with the glycosylation of cellular receptors of SARS-CoV[4].

Chloroquine/氯喹 細胞實驗

Cell Line
Concentration Treated Time Description References
Werner syndrome-specific mesenchymal stem cells (WS hMSCs) 0.2 μM to 100 μM Low concentrations of CQ (0.2-5 μM) promoted cell self-renewal, while higher concentrations (20 μM or above) inhibited cell proliferation. Treatment with 1 μM CQ decreased the percentage of SA-β-gal-positive cells and increased the number of Ki67-positive cells, while also reducing IL-6 secretion. Protein Cell. 2022 Jun;13(6):454-461.
U2OS cells expressing GFP-TFEB fusion protein 0.1, 0.3, 1, 3, 10, 30 μM 6 h Triggered TFEB nuclear translocation Cell Death Dis. 2021 Jan 6;12(1):6.
Human glioma H4 cells 10, 20, 40 μM 6 h Induced GFP-LC3 dot formation, indicating autophagosome accumulation Cell Death Dis. 2021 Jan 6;12(1):6.
Human U2OS osteosarcoma cells 10, 20, 40 μM 6 h Induced GFP-LC3 dot formation, indicating autophagosome accumulation Cell Death Dis. 2021 Jan 6;12(1):6.
A549 71.3 ± 6.1 μM Induced apoptosis, suppressed autophagy Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
H460 55.6 ± 12.5 μM Induced apoptosis, suppressed autophagy Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
H1299 50 μM Inhibited autophagy, decreased transcriptional activity and disrupted the localization of p53-R273H Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
A549 2.5 ~ 60 μM Blocked the PI3K/AKT signaling pathway, mediated mitochondrial apoptosis and inhibited autophagy Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MCF-7 20 μM Inhibition of autophagy/mitophagy, induced apoptosis Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
BT549 20 μM Inhibition of autophagy/mitophagy, induced apoptosis Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MDA-MB-231 20 μM Inhibition of autophagy/mitophagy, induced apoptosis Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
MiaPaca-2 100 μM 72 h Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
MiaPaca-1 100 μM 72 h Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
AsPC-1 100 μM 72 h Assess the cytotoxicity of CQ-HES, results showed similar cytotoxicity between CQ-HES and HCQ Biomacromolecules. 2017 Aug 14;18(8):2247-2257.
Calu-3 cells 64.7 μM (CQ), 119 μM (HCQ) To study the inhibitory effect of CQ and HCQ on SARS-CoV-2 infection, results showed that the effective dose in Calu-3 cells was significantly higher than in Vero E6 cells. J Mol Cell Biol. 2021 Jul 6;13(3):175-184.
Vero E6 cells 6.5 μM To study the inhibitory effect of CQ and HCQ on SARS-CoV-2 infection, results showed that CQ and HCQ effectively inhibited viral invasion in Vero E6 cells. J Mol Cell Biol. 2021 Jul 6;13(3):175-184.

Chloroquine/氯喹 動物實驗

Species
Animal Model
Administration Dosage Frequency Description References
Mice HCT116 human colon carcinoma xenografts Intraperitoneal injection 20 mg/kg Every second day for 16 days Evaluate the inhibitory effect of CQ on tumor growth, results showed CQ as a single-agent treatment had no significant effect on tumor growth Autophagy. 2014 Apr;10(4):562-71
C57BL/6J mice Nilotinib-induced nephrotoxicity model Intragastric administration 30 mg/kg Daily for 30 days To investigate the intervention effect of chloroquine on nilotinib-induced nephrotoxicity. The results showed that chloroquine significantly ameliorated nilotinib-induced renal injury, reduced blood urea nitrogen and serum creatinine levels, and decreased renal fibrosis. Adv Sci (Weinh). 2023 Sep;10(26):e2302002.
Sprague Dawley (SD) rats 24-month-old rats Oral 0.1 mg/kg Twice a week for 5 months Low-dose CQ treatment extended the lifespan of rats, repressed systemic inflammation, and inhibited fibrosis across multiple tissues. CQ treatment also reduced serum TNF-α levels and the numbers of circulating white blood cells and neutrophils, indicating attenuated chronic inflammation. Protein Cell. 2022 Jun;13(6):454-461.
Mice C57Bl/6j mice Intraperitoneal injection 50 mg/kg Once daily for 10 days Detected eIF2α phosphorylation levels, indicating that HCQ can induce eIF2α phosphorylation in vivo Cell Death Dis. 2021 Jan 6;12(1):6.
Mouse Breast cancer model Intraperitoneal injection 40 mg/kg Once every two days Inhibition of autophagy/mitophagy, induced apoptosis Int J Nanomedicine. 2024 Jul 5;19:6777-6809.
Mice HCoV-OC43 infection model 15 mg/kg To study the preventive effect of CQ on HCoV-OC43 infection, results showed that 15 mg/kg of CQ effectively prevented infection in mice. J Mol Cell Biol. 2021 Jul 6;13(3):175-184.

Chloroquine/氯喹 參考文獻

[1]Said A, Bock S, Lajqi T, Müller G, Weindl G. 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, Sandholm J, Kauppila JH, Lehenkari P, Harris KW, Selander KS. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672

[3]Xue J, Moyer A, Peng B, Wu J, Hannafon BN, Ding WQ. Chloroquine is a zinc ionophore. PLoS One. 2014 Oct 1;9(10):e109180

[4]Colson P, Rolain JM, Lagier JC, Brouqui P, Raoult D. Chloroquine and hydroxychloroquine as available weapons to fight COVID-19. Int J Antimicrob Agents. 2020 Apr;55(4):105932

Chloroquine/氯喹 實驗方案

計算器
存儲液制備 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.63mL

3.13mL

1.56mL

31.26mL

6.25mL

3.13mL

Chloroquine/氯喹 技術信息

CAS號54-05-7
分子式C18H26ClN3
分子量 319.87
SMILES Code CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC
MDL No. MFCD00024009
別名 NSC-187208; CHQ; CQ
英文名稱N4-(7-Chloroquinolin-4-yl)-N1,N1-diethylpentane-1,4-diamine
運輸藍冰
InChI Key WHTVZRBIWZFKQO-UHFFFAOYSA-N
Pubchem ID 2719
存儲條件

In solvent -20°C: 3-6個月 -80°C: 12個月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO 中的溶解度 : 200 mg/mL (625.25 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

Ethanol 中的溶解度 : 100 mg/mL (312.63 mM; 超聲助溶)

請根據您的動物給藥指南選擇適當的溶解方案。
以下溶解方案都請先按照體外實驗的方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議現用現配，當天使用； 以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶
方案 一
方案 二
方案 三
配制的工作液建議現用現配，短期內盡快用完。 以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶。
方案 一
方案 二
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