Hydroxychloroquine (HCQ) Sulfate

製品コードS4430 バッチS443008

化学情報

	Synonyms	NSC 4375	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₂₈ClN₃O₅S
	分子量	433.95	CAS No.	747-36-4
Solubility (25°C)*	体外	Water	87 mg/mL (200.48 mM)
		DMSO	Insoluble
		Ethanol	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
in vitro	Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis^[2].
in vivo	The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent^[3]. In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals^[4].

製品説明

Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.

in vitro

Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis^[2].

in vivo

The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent^[3].

In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals^[4].

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro kinase assays
キナーゼアッセイ	with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.
細胞アッセイ	細胞株	Human RCC cell lines
	濃度	75 or 100 μM
	反応時間	48 h
	実験の流れ	All cells are cultured in RPMI with 10% FBS, 1% glutamine, and 1% Pen/Strep. cells are seeded on the appropriated plates overnight and treated with HCQ (75 or 100 μM) for 48 hours.
動物実験	動物モデル	Male Sprague Dawley (SD) rats
	投薬量	200 mg/kg
	投与方法	oral administration

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1489]

: Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):272]

: Data from [Data independently produced by , , Cell Death Dis, 2017, 8(1):e2558]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Acetylation of MOB1 mediates polyphyllin II-reduced lysosome biogenesis in breast cancer by promoting the cytoplasmic retention of the YAP/TFEB coactivator complex [ Phytomedicine, 2024, 10.1016/j.phymed.2023.155152]	PubMed: 37922793
ATG7/GAPLINC/IRF3 axis plays a critical role in regulating pathogenesis of influenza A virus [ PLoS Pathog, 2024, 20(1):e1011958]	PubMed: 38227600
The nucleotide-sensing Toll-Like Receptor 9/Toll-Like Receptor 7 system is a potential therapeutic target for IgA nephropathy [ Kidney Int, 2023, 104(5):943-955]	PubMed: 37648155
Single-cell sequencing of ascites fluid illustrates heterogeneity and therapy-induced evolution during gastric cancer peritoneal metastasis [ Nat Commun, 2023, 14(1):822]	PubMed: 36788228
AR antagonists develop drug resistance through TOMM20 autophagic degradation-promoted transformation to neuroendocrine prostate cancer [ J Exp Clin Cancer Res, 2023, 42(1):204]	PubMed: 37563661
Combination Therapies with CDK4/6 Inhibitors to Treat KRAS-Mutant Pancreatic Cancer [ Cancer Res, 2023, 83(1):141-157]	PubMed: 36346366
Tetrandrine synergizes with MAPK inhibitors in treating KRAS-mutant pancreatic ductal adenocarcinoma via collaboratively modulating the TRAIL-death receptor axis [ Pharmacol Res, 2023, 197:106955]	PubMed: 37820855
Platelet factor 4 limits neutrophil extracellular trap- and cell-free DNA-induced thrombogenicity and endothelial injury [ JCI Insight, 2023, 8(22)e171054]	PubMed: 37991024
PSGL-1 is an evolutionarily conserved antiviral restriction factor [ mBio, 2023, 10.1128/mbio.00387-23]	PubMed: 37787515
Piperine Induces Apoptosis and Autophagy in HSC-3 Human Oral Cancer Cells by Regulating PI3K Signaling Pathway [ Int J Mol Sci, 2023, 24(18)13949]	PubMed: 37762259

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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