1. Immunology/Inflammation
    Autophagy
  2. Toll-like Receptor (TLR)
    Autophagy

Chloroquine diphosphate 

Cat. No.: HY-17589 Purity: 99.94%
Handling Instructions

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

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

Chloroquine diphosphate Chemical Structure

Chloroquine diphosphate Chemical Structure

CAS No. : 50-63-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 73 In-stock
Estimated Time of Arrival: December 31
100 mg USD 66 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

    Chloroquine diphosphate 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 diphosphate 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 diphosphate 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 diphosphate purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 May 19;18(5). pii: E1063.

    Inhibition of sirt1 and AMPK blocked Rb2-induced hepatic autophagy. HepG2 cells are pretreated with 50 µM Rb2 for 4 h in the presence or absence of the sirt1 inhibitor EX-528 (EX) and the specific AMPK inhibitor Compound C (CC), and then subjected to OA (1 mM for HepG2 and 2 mM for primary mouse hepatocytes) exposure for 12 h. For lipid content determination, intracellular TG are stained by Oil red O (ORO). ORO is then eluted with isopropanol and the optical absorbance of the eluate is measured

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

    Caspase signaling pathway. MCF7 and MDA-MB-231 cells are pretreated with 10 µM Z-VAD-FMK and BOC-D-FMK for 1 h and then exposed to 80 μM ω3-FFAs and 20 μM ATRA for 48 h. The expression of PARP protein.

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

    Autophagy is involved in Rg1-inhibited apoptosis in macrophages Macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in the absence or presence of 3-MA (5 mM). The protein expression level of cleaved caspase-3 determined by western blot analysis in Raw264.7 macrophages.

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

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.

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

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

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

    Cell morphology of MCF-7 treated with RA (20 μM)+ω-3 PUFAs (80 μM) with or without 3-MA (5 mM) for 24h.

    Chloroquine diphosphate 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 diphosphate purchased from MCE. Usage Cited in: Chem Biol Interact. 2018 Mar 1;283:59-74.

    The expression levels of apoptosis-associated proteins after treatment with morusin or tumor necrosis factor-alpha (TNF-α)/Cycloheximide (CHX). A2780 cells are incubated with the indicated concentrations of morusin or TNF-α (50 ng/mL)/CHX (50 μM) for 24 h. GAPDH is used as a loading control in western blot analysis.

    Chloroquine diphosphate purchased from MCE. Usage Cited in: Chem Biol Interact. 2018 Mar 1;283:59-74.

    The expression levels of apoptosis-associated proteins after treatment with morusin or tumor necrosis factor-alpha (TNF-α)/Cycloheximide (CHX). SKOV-3 cells are incubated with the indicated concentrations of morusin or TNF-α (50 ng/mL)/CHX (50 μM) for 24 h. GAPDH is used as a loading control in western blot analysis.

    Chloroquine diphosphate 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 Celecoxib (Cel, 5-40 μM) for 24 h. Celecoxib decreases protein expression of COX-2 compared with control as indicated by western blot.

    Chloroquine diphosphate 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 diphosphate 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 diphosphate 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 diphosphate purchased from MCE. Usage Cited in: Neurosci Lett. 2018 Jun 18;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 diphosphate purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    Cells are pretreated with 5 mM 3-MA or 2 μM for 1 h and then exposed to 40 μM EPA and 10 μM Rp for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Chloroquine diphosphate 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 diphosphate 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 diphosphate purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5311-5321.

    The expression of PI3K, Akt, p-Akt, HO-1, LC3-II/LC3-I and Beclin-1 in LY294002 group after pharmorubicin treatment are examined by Western blot. The protein expression in LY294002 group is decreased.

    Chloroquine diphosphate purchased from MCE. Usage Cited in: Prostate. 2018 Sep 3.

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

    Cells are treated with AICAR and AICAR (A++, 10 μM) + Compound C (C++, 1 μM) for 24 h, after which western blot analysis is performed.

    Chloroquine diphosphate 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    Autophagy, TLRs[1][2][3]

    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 (CHQ, 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].

    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].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 33 mg/mL (63.97 mM)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9385 mL 9.6926 mL 19.3851 mL
    5 mM 0.3877 mL 1.9385 mL 3.8770 mL
    10 mM 0.1939 mL 0.9693 mL 1.9385 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    The cells are cultured in 6-well plates with normal culture medium in the presence of vehicle or 25 or 50 μM chloroquine, until near confluency, after which they are rinsed with sterile phosphate-buffered saline (PBS) and cultured further for the indicated times in serum-free culture medium. At the desired time-points, the culture medium is discarded and the cells are quickly harvested in lysis buffer and clarified by centrifugation. Subsequent to boiling the supernatants in reducing sodium dodecyl sulphate (SDS) sample buffer, equal amounts of protein (100 μg) are loaded per lane and the samples are electrophoresed into 10 or 4-20% gradient polyacrylamide SDS gels, then transferred to a nitrocellulose membrane. To detect TLR9, the blots are incubated overnight at 4°C with anti-TLR9 antibodies, diluted 1:500 in Tris-buffered saline with 0.1% (v/v) Tween-20 (TBST). Equal loading is confirmed with polyclonal rabbit anti-actin. Secondary detection is performed with horseradish peroxidase-linked secondary antibodies. The protein bands are visualized by chemiluminescence using an ECL kit.

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

    Animal Administration
    [2]

    Control and TLR9 siRNA MDA-MB-231 cells (5×105 cells in 100 μL) are inoculated into the mammary fat pads of four-week-old, immune-deficient mice (athymic nude/nu Foxn1). Treatments are started seven days after tumor cell inoculation. The mice are treated daily either with intraperitoneal (i.p.) chloroquine (80 mg/kg) or vehicle (PBS). The animals are monitored daily for clinical signs. Tumor measurements are performed twice a week and tumor volume is calculated according to the formula V=(π/6) (d1×d2)3/2, where d1 and d2 are perpendicular tumor diameters. The tumors are allowed to grow for 22 days, at which point the mice are sacrificed and the tumors are dissected for a final measurement. Throughout the experiments, the animals are maintained under controlled pathogen-free environmental conditions (20-21°C, 30-60% relative humidity and a 12-h lighting cycle). The mice are fed with small-animal food pellets and supplied with sterile water ad libitum.

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

    References
    Molecular Weight

    515.86

    Formula

    C₁₈H₃₂ClN₃O₈P₂

    CAS No.

    50-63-5

    SMILES

    O=P(O)(O)O.O=P(O)(O)O.CC(NC1=CC=NC2=CC(Cl)=CC=C12)CCCN(CC)CC

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.94%

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Chloroquine diphosphate
    Cat. No.:
    HY-17589
    Quantity:

    Chloroquine diphosphate

    Cat. No.: HY-17589