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  3. Chloroquine dihydrochloride

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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Customer Review

Based on 693 publication(s) in Google Scholar

Other Forms of Chloroquine dihydrochloride:

Top Publications Citing Use of Products

676 Publications Citing Use of MCE Chloroquine dihydrochloride

WB
Proliferation Assay
IF

    Chloroquine dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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).
    • Biological Activity

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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[1][2][3][5]

    Plasmodium

     

    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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    392.79

    Formula

    C18H28Cl3N3

    CAS No.
    Appearance

    Oil

    Color

    Light yellow to yellow

    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

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (254.59 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5459 mL 12.7294 mL 25.4589 mL
    5 mM 0.5092 mL 2.5459 mL 5.0918 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Purity & Documentation
    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 (sealed storage, away from moisture and 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
    H2O 1 mM 2.5459 mL 12.7294 mL 25.4589 mL 63.6472 mL
    5 mM 0.5092 mL 2.5459 mL 5.0918 mL 12.7294 mL
    10 mM 0.2546 mL 1.2729 mL 2.5459 mL 6.3647 mL
    15 mM 0.1697 mL 0.8486 mL 1.6973 mL 4.2431 mL
    20 mM 0.1273 mL 0.6365 mL 1.2729 mL 3.1824 mL
    25 mM 0.1018 mL 0.5092 mL 1.0184 mL 2.5459 mL
    30 mM 0.0849 mL 0.4243 mL 0.8486 mL 2.1216 mL
    40 mM 0.0636 mL 0.3182 mL 0.6365 mL 1.5912 mL
    50 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2729 mL
    60 mM 0.0424 mL 0.2122 mL 0.4243 mL 1.0608 mL
    80 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7956 mL
    100 mM 0.0255 mL 0.1273 mL 0.2546 mL 0.6365 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Chloroquine dihydrochloride
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