1. Autophagy
    Immunology/Inflammation
    Anti-infection
  2. Parasite
    Autophagy
    SARS-CoV
    Toll-like Receptor (TLR)
    HIV
    Antibiotic
  3. Chloroquine dihydrochloride

Chloroquine dihydrochloride 

Cat. No.: HY-17589B
Handling Instructions

Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).

For research use only. We do not sell to patients.

Chloroquine dihydrochloride Chemical Structure

Chloroquine dihydrochloride Chemical Structure

CAS No. : 3545-67-3

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Top Publications Citing Use of Products

Publications Citing Use of MCE Chloroquine dihydrochloride

    Chloroquine dihydrochloride purchased from MCE. Usage Cited in: Tumour Biol. 2016 Jul;37(7):8811-24.

    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).

    Chloroquine dihydrochloride purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.

    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 dihydrochloride purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2016 Dec;48(12):1075-1084.

    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 dihydrochloride purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    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 dihydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    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 dihydrochloride purchased from MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.

    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 dihydrochloride purchased from MCE. Usage Cited in: Oncogene. 2018 May;37(22):2936-2952.

    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 dihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):501-507.

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

    Chloroquine dihydrochloride purchased from MCE. Usage Cited in: Neurosci Lett. 2018 Aug 24;682:112-117.

    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 dihydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    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 dihydrochloride purchased from MCE. Usage Cited in: J Pharmacol Exp Ther. 2018 Oct;367(1):20-27.

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

    Chloroquine dihydrochloride purchased from MCE. Usage Cited in: Prostate. 2019 Jan;79(1):44-53.

    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 dihydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Dec;109:1617-1627.

    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 dihydrochloride purchased from MCE. Usage Cited in: EBioMedicine. 2017 May;19:49-59.

    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 dihydrochloride purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.

    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.
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    Description

    Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride 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

    Malaria

     

    TLRs

     

    SARS-COV-2

     

    HIV-1

     

    In Vitro

    Chloroquine dihydrochloride (20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine dihydrochloride (20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4+ T cells[1]. Chloroquine dihydrochloride (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine dihydrochloride 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 dihydrochloride significantly reduces HuH7 cell proliferation in vitro[3].
    Chloroquine dihydrochloride (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 dihydrochloride 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].

    In Vivo

    Chloroquine dihydrochloride (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 dihydrochloride significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by Chloroquine[3].

    Molecular Weight

    392.79

    Formula

    C₁₈H₂₈Cl₃N₃

    CAS No.

    3545-67-3

    SMILES

    CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    ChloroquineParasiteAutophagySARS-CoVToll-like Receptor (TLR)HIVAntibioticSARS coronavirusHuman immunodeficiency virusmalariainflammatoryrheumatoidarthritisSARS-CoV-2COVID-19infectionimmune-modulatingInhibitorinhibitorinhibit

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    Product Name:
    Chloroquine dihydrochloride
    Cat. No.:
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