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  3. Chloroquine

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 is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).

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Chloroquine Chemical Structure

Chloroquine Chemical Structure

CAS No. : 54-05-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 568 publication(s) in Google Scholar

Other Forms of Chloroquine:

Top Publications Citing Use of Products

551 Publications Citing Use of MCE Chloroquine

WB
Proliferation Assay
IF

    Chloroquine purchased from MedChemExpress. Usage Cited in: Immun Inflamm Dis. 2023 Apr 12; 11:e830.

    Chloroquine (10 μM; 30 min) reverses the effect of OmpA on autophagy by inhibiting the expression of LC3 in BMDCs.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Immun Inflamm Dis. 2023 Apr 12; 11:e830.

    Chloroquine (10 μM; 30 min) reverses the effect of OmpA on autophagy by inhibiting the expression of Beclin1 and LC3II/I while increasing the expression of P62 in BMDCs.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Prostate. 2019 Jan;79(1):44-53.  [Abstract]

    Treatment with sub-dose of Everolimus (10 nM), together with CQ (5 µM) increases the levels of Bax and cleaved PARP, and decreases the levels of Bcl-2 expression in both PC3 and LNPER cells.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 May;37(22):2936-2952.  [Abstract]

    IPZ-treated U87 and U251 cells are treated with or without Baf-A1 (5 nM), CQ (40 μM), or MG132 (1 μM) for 48 h, followed by western blots.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Dec;109:1617-1627.  [Abstract]

    GFP-LC3B-expressing LX-2 cells are treated with DMSO, 3-MA (10 mM), or Chloroquine (30 μM) alone or in the presence of Carvedilol (CVD, 10 μM) for 24 h. The conversion of LC3B-I to LC3B-II is evaluated using immunoblotting.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.  [Abstract]

    MC3T3-E1 cells are treated with AICAR (10 μM) in the presence or absence of 3-MA (5 mM) or CQ (10 μM) for 24 h, after which western blot analysis is conducted.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.  [Abstract]

    L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.  [Abstract]

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Chloroquine purchased from MedChemExpress. Usage Cited in: J Pharmacol Exp Ther. 2018 Oct;367(1):20-27.  [Abstract]

    Protein expression of LC3B and p62 in Panc-1 cells treated with Carboxamidotriazole (CAI) and/or Chloroquine (CQ).

    Chloroquine purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):501-507.  [Abstract]

    Western blot analysis of autophagy markers and LAMP2 in mice with AAV-vaspin and Chloroquine (CQ) pretreatment after I/R (1d).

    Chloroquine purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2018 Aug 24;682:112-117.  [Abstract]

    After treatment of CDDP with or without the autophagy inhibitor CQ, the expression of LC3-II in the CQ+CDDP group is less than that in the CQ group but is higher than that in the CDDP group at 24 h and 96 h.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.  [Abstract]

    Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Chloroquine purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2017 May;19:49-59.  [Abstract]

    mCherry-GFPLC3 puncta analysis in SPC-A-1 cells. Cells are transfected with mCherry-GFP-LC3 plasmid and incubated for 6 h. Next, cells are pretreated with or without Chloroquine (50 μM) for 1 h followed by stimulation of 5 μM Flu for 24 h or 36 h. Scale bar, 10 μm and 2 μm (magnified graph). The lysosomal inhibitor Chloroquine (CQ) raises the lysosomal pH and increases the autophagic flux.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.  [Abstract]

    p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80 μM ω-3 FFAs, 20 μM ATRA alone or in combination for 48 h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.  [Abstract]

    Cells are treated with RA (20 μM) plus ω-3 PUFAs (80 μM) with or without CQ (5 μM) for 24 h. Cell extracts are prepared and subjected to western blotting analysis.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2016 Dec;48(12):1075-1084.  [Abstract]

    The change of LC3 is analyzed by western blotting after 6 h hypoxia in the presence or absence of Chloroquine of WDR26-overexpressing H9c2 cells.

    Chloroquine purchased from MedChemExpress. Usage Cited in: Tumour Biol. 2016 Jul;37(7):8811-24.  [Abstract]

    Assays for autophagy activity. Immunoblot analysis for LC3B. Compared with the Lenti-NC cells, the Lenti-CD44v6 cells display a higher intensity of autophagy flux but not steady-state levels when treated with 5-FU (*P<0.001).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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 is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].

    IC50 & Target[1][2][3][5]

    Plasmodium

     

    Malaria

     

    TLRs

     

    SARS-COV-2

     

    HIV-1

     

    In Vitro

    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 (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 IRS-954 or chloroquine significantly reduces HuH7 cell proliferation in vitro[3].
    Chloroquine (0.01-100 μM; 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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 IRS-954 or chloroquine significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by Chloroquine[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    319.87

    Formula

    C18H26ClN3

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    Ethanol : 100 mg/mL (312.63 mM; Need ultrasonic)

    DMSO : 50 mg/mL (156.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1263 mL 15.6314 mL 31.2627 mL
    5 mM 0.6253 mL 3.1263 mL 6.2525 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (31.26 mM); Suspended solution; Need ultrasonic and warming and heat to 44°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.82%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
    15 mM 0.2084 mL 1.0421 mL 2.0842 mL 5.2105 mL
    20 mM 0.1563 mL 0.7816 mL 1.5631 mL 3.9078 mL
    25 mM 0.1251 mL 0.6253 mL 1.2505 mL 3.1263 mL
    30 mM 0.1042 mL 0.5210 mL 1.0421 mL 2.6052 mL
    40 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9539 mL
    50 mM 0.0625 mL 0.3126 mL 0.6253 mL 1.5631 mL
    60 mM 0.0521 mL 0.2605 mL 0.5210 mL 1.3026 mL
    80 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9770 mL
    100 mM 0.0313 mL 0.1563 mL 0.3126 mL 0.7816 mL
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    Product Name:
    Chloroquine
    Cat. No.:
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