1. GPCR/G Protein Neuronal Signaling Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Cannabinoid Receptor Apoptosis Reactive Oxygen Species (ROS)
  3. CB2R agonist 4

CB2R agonist 4 是一种大麻素受体 2 (CB2R) 激动剂,EC50 值为 6.9 μM。CB2R agonist 4 可诱导细胞凋亡 (apoptosis)、活性氧 (ROS) 产生和蛋白质错误折叠。CB2R agonist 4 对多种肿瘤细胞具有细胞毒性。CB2R agonist 4 可用于癌症研究。

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CB2R agonist 4

CB2R agonist 4 Chemical Structure

CAS No. : 182496-82-8

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生物活性

CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. CB2R agonist 4 can induce cell apoptosis, ROS production and protein misfolding. CB2R agonist 4 shows cytotoxicity to a panel of tumor cell lines. CB2R agonist 4 can be used for the research of cancer[1].

IC50 & Target[1]

CB2R

6.9 μM (EC50)

体外研究
(In Vitro)

CB2R agonist 4 (Compound 63) 对 HaCaT、HEPG2、A375、SHSY5Y、MCF7 和 A549 细胞具有细胞毒性,其 EC50 值分别为 21.41、2.17、2.29、23.21、27.93 和 36.4 μM[1]
CB2R agonist 4 对 TRPM8 和 BRD4 有显著抑制作用,IC50 值为 0.36 μM 和 0.11 μM,对 BRK 的抑制作用较弱,IC50 值为 29.17 μM,并且能激活 TRPA1,EC50 值为 2.54 μM[1]
CB2R agonist 4 在 A357 细胞中诱导脂质重塑,表现为二酰甘油、胆固醇酯减少,溶血磷脂酰胆碱、溶血磷脂酰乙醇胺增加[1]
CB2R agonist 4 (2.5-10 μM, 2-8 h) 在 A357 细胞中诱导活性氧 (ROS) 产生[1]
CB2R agonist 4 (5-20 μM, 24 h) 会增加 A357 细胞中错误折叠蛋白的水平[1]
CB2R agonist 4 (1.25-5 μM, 72 h) 会诱导 A357 细胞凋亡[1]

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

Immunofluorescence[1]

Cell Line: A357 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 24 h
Result: Showed the greatest increase in fluorescence at 20 μM.
分子量

366.41

Formula

C21H22N2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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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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CB2R agonist 4
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