Chloroquine

Catalog No.S6999 Batch:S699902

Technical Data

Formula	C₁₈H₂₆ClN₃
Molecular Weight	319.87	CAS No.	54-05-7
Solubility (25°C)*	In vitro	DMSO	64 mg/mL (200.08 mM)
		Ethanol	64 mg/mL (200.08 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.

Targets

Autophagy ^[1]	lysosome ^[1]	TLR9 ^[2]	HIV-1 ^[4]	SARS-CoV-2 ^[3] (Vero E6 cells based assay)
				1.13 μM(EC50)

In vitro

Chloroquine is a widely used autophagy inhibitor.^[5]

In vivo

The inhibition of autophagy by chloroquine potentiates the therapeutic effect of PI3K/AKT inhibitors in vitro and in vivo TNBC models, synergizing with taxane-based chemotherapy.^[6]

Protocol (from reference)

Cell Assay:^{^[5]}	Cell lines HL‐60 cells Concentrations 10 µM Incubation Time 48 h Method One day before treatment, AML cells were seeded with a density of 2 × 10⁵ cells/mL. Fresh medium containing different concentrations of Ara‐C was added into the culture medium. Cells were further cultured for 24 or 48 h based on experimental purposes. For inhibition of autophagy, HL‐60 cells were treated with 200 nM bafilomycin A1 or 10 µM chloroquine. Overexpression and knockdown were performed by transfection. (Data sourced from selleck products)
Animal Study:^{^[6]}	Animal Models Female NOD/SCID athymic mice injected with MDAMB231 cells Dosages 30 mg/kg Administration o.g. (Data sourced from selleck products)

Cell Assay:^{^[5]}

Cell lines
HL‐60 cells
Concentrations
10 µM
Incubation Time
48 h
Method
One day before treatment, AML cells were seeded with a density of 2 × 10⁵ cells/mL. Fresh medium containing different concentrations of Ara‐C was added into the culture medium. Cells were further cultured for 24 or 48 h based on experimental purposes. For inhibition of autophagy, HL‐60 cells were treated with 200 nM bafilomycin A1 or 10 µM chloroquine. Overexpression and knockdown were performed by transfection.

(Data sourced from selleck products)

Animal Study:^{^[6]}

Animal Models
Female NOD/SCID athymic mice injected with MDAMB231 cells
Dosages
30 mg/kg
Administration
o.g.

(Data sourced from selleck products)

References

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Selleck's Chloroquine has been cited by 184 publications

Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer [ Signal Transduct Target Ther, 2024, 9(1):65]	PubMed: 38461173
Combined targeting of GPX4 and BCR-ABL tyrosine kinase selectively compromises BCR-ABL+ leukemia stem cells [ Mol Cancer, 2024, 23(1):240]	PubMed: 39465372
Engineered a dual-targeting HA-TPP/A nanoparticle for combination therapy against KRAS-TP53 co-mutation in gastrointestinal cancers [ Bioact Mater, 2024, 32:277-291]	PubMed: 37876556
SLC13A3 is a major effector downstream of activated β-catenin in liver cancer pathogenesis [ Nat Commun, 2024, 15(1):7522]	PubMed: 39215042
Autophagy regulates the maturation of hematopoietic precursors in the embryo [ Nat Commun, 2024, 15(1):2255]	PubMed: 38490977
Targeting autophagy overcomes cancer-intrinsic resistance to CAR-T immunotherapy in B-cell malignancies [ Cancer Commun (Lond), 2024, 44(3):408-432]	PubMed: 38407943
Blockade of the deubiquitinating enzyme USP48 degrades oncogenic HMGA2 and inhibits colorectal cancer invasion and metastasis [ Acta Pharm Sin B, 2024, 14(4):1624-1643]	PubMed: 38572092
Dysregulated CREB3 cleavage at the nuclear membrane induces karyoptosis-mediated cell death [ Exp Mol Med, 2024, 56(3):686-699]	PubMed: 38480902
FUNDC1 alleviates doxorubicin-induced cardiotoxicity by restoring mitochondrial-endoplasmic reticulum contacts and blocked autophagic flux [ Theranostics, 2024, 14(9):3719-3738]	PubMed: 38948070
Synthetic lethality of combined ULK1 defection and p53 restoration induce pyroptosis by directly upregulating GSDME transcription and cleavage activation through ROS/NLRP3 signaling [ J Exp Clin Cancer Res, 2024, 43(1):248]	PubMed: 39215364

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SHIPPING AND STORAGE
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