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- 2025年12月26日
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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Acetylshikonin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
24502-78-1
- 规格：
10mg/5mg
| 规格： | 10mg | 产品价格： | ￥1190.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥740.0 |
是一种非选择性的细胞色素 P450 抑制剂和 AChE 抑制剂，具有很强的抗凋亡活性。
| 基本信息 | |
| CAS | No.24502-78-1 |
| 中文名称 | 乙酰紫草素 |
| 英文名称 | Acetylshikonin |
| 别名 | O-Acetylshikonin |
| 分子式 | C18H18O6 |
| 分子量 | 330.33 |
| 溶解性 | Soluble in DMSO |
| 纯度 | HPLC≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00143538 |
| SMILES | O=C1C([C@H](OC(C)=O)C/C=C(C)\C)=CC(C2=C1C(O)=CC=C2O)=O |
| InChIKey | WNFXUXZJJKTDOZ-OAHLLOKOSA-N |
| InChI | InChI=1S/C18H18O6/c1-9(2)4-7-15(24-10(3)19)11-8-14(22)16-12(20)5-6-13(21)17(16)18(11)23/h4-6,8,15,20-21H,7H2,1-3H3/t15-/m1/s1 |
| PubChem CID | 479501 |
| 靶点 | Cytochrome P450 |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | 是一种非选择性的细胞色素 P450 抑制剂和 AChE 抑制剂,具有很强的抗凋亡活性。 |
| 生物活性 | Acetylshikonin， derived from the root of Lithospermum erythrorhizon， has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity[1-3]. |
| In Vitro | Acetylshikonin inhibited CYP2J2-mediated astemizole O-demethylation activity(Ki = 2.1μM)in a noncompetitive manner. The noncompetitive inhibitory effect of acetylshikonin on CYP2J2 enzyme was also demonstrated using this 3D structure，which showed different binding location of astemizole and acetylshikonin in CYP2J2 model. It showed cytotoxic effects against human hepatoma HepG2 cells(IC50 = 2μM). In addition，acetylshikonin treatment inhibited growth of human hepatocellular carcinoma HepG2 cells leading to apoptosis accompanied with p53，bax，and caspase3 activation as well as bcl2 down-regulation.[1] Acetylshikonin showed a strong inhibitory effect against all P450s tested with IC50 values of 1.4-4.0 μ m.. Acetylshikonin may be a novel general P450 inhibitor，which could replace SKF-525A.[2] Acetylshikonin，a Novel AChE Inhibitor，Inhibits Apoptosis via Upregulation of Heme Oxygenase-1 Expression in SH-SY5Y Cells[3]. |
| 细胞实验 | Astemizole，a representative CYP2J2 probe substrate，was incubated in HLMs in the presence or absence of acetylshikonin. After incubation，the samples were analyzed by liquid chromatography and triple quadrupole mass spectrometry. The anti-cancer activity of acetylshikonin was evaluated on human hepatocellular carcinoma HepG2 cells. WST-1，cell counting，and colony formation assays were further adopted for the estimation of the growth rate of HepG2 cells treated with acetylshikonin.[1] |
| 数据来源文献 | [1]. Park SH， et al. Identification of acetylshikonin as the novel CYP2J2 inhibitor with anti-cancer activity in HepG2 cells. Phytomedicine. 2017 Jan 15;24:134-140. [2]. Shon JC， et al. Acetylshikonin is a novel non-selective cytochrome P450 inhibitor. Biopharm Drug Dispos. 2017 Dec;38(9):553-556. [3]. Wang Y， et al. Acetylshikonin， a Novel AChE Inhibitor， Inhibits Apoptosis via Upregulation of Heme Oxygenase-1 Expression in SH-SY5Y Cells. Evid Based Complement Alternat Med. 2013;2013:937370. |
| 单位 | 瓶 |
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IA1180 乙酰紫草素 代谢酶/蛋白酶 索莱宝
￥740 - 1190
