Chloroquine dihydrochloride

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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

CAS No. : 3545-67-3

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Other In-stock Forms of Chloroquine dihydrochloride:

Chloroquine phosphate Chloroquine Chloroquine-d₅

Other Forms of Chloroquine dihydrochloride:

529 Publications Citing Use of MCE Chloroquine dihydrochloride

Proliferation Assay

: 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).

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Said A, et al. 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. [Content Brief]

[2]. Tuomela J, et al. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672. [Content Brief]

[3]. Mohamed FE, et al. Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2014 Jul 2. doi: 10.1111/liv.12626. [Content Brief]

[4]. Colson P, et al. Chloroquine and hydroxychloroquine as available weapons to fight COVID-19. Int J Antimicrob Agents. 2020;55(4):105932. [Content Brief]

[5]. Savarino A, et al. The anti-HIV-1 activity of chloroquine. J Clin Virol. 2001;20(3):131-135. [Content Brief]