Acetylshikonin是一种从紫草(Lithosperraum erythrorhizon Sieb. et Zucc.)根中分离纯化的天然产物,它抑制中性粒细胞激活过程中的 NADPH 氧化酶复合体生成,但不会直接抑制已生成的 NADPH 氧化酶活性,同时也是一种非选择性细胞色素 P450 抑制剂。


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| 产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
95% | |||||||||||||||||
| Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
| PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
| MRT68921 HCl |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
| ROC-325 | ✔ | 99%+ | |||||||||||||||||
| Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
| Lys05 | ✔ | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Acetyl shikonin, a natural product isolated and purified from the roots of Lithosperraum erythrorhizon Sieb. et Zucc., inhibits the generation of NADPH oxidase complex in the activation of respiratory burst of PMNs, but does not directly inhibit the activity of NADPH oxidase already generated, and is a non-selective cytochrome P450 inhibitor. |
| Concentration | Treated Time | Description | References | |
| HCT-15 | HCT-15 | 24, 48, 72 h | Suppressed cell proliferation by inducing G1 phase cell cycle arrest and apoptosis | Br J Pharmacol. 2020 May;177(10):2303-2319. |
| HCT-116 | HCT-116 | 24, 48, 72 h | Suppressed cell proliferation by inducing G2 phase cell cycle arrest and apoptosis | Br J Pharmacol. 2020 May;177(10):2303-2319. |
| SW 620 | SW 620 | 24, 48, 72 h | Suppressed cell proliferation by inducing G3 phase cell cycle arrest and apoptosis | Br J Pharmacol. 2020 May;177(10):2303-2319. |
| DLD-1 | DLD-1 | 24, 48, 72 h | Suppressed cell proliferation by inducing G4 phase cell cycle arrest and apoptosis | Br J Pharmacol. 2020 May;177(10):2303-2319. |
| Lung single cells | Lung single cells | 12 h | Acetylshikonin down-regulated the production of IL-6 in a dose-dependent manner, with significant reduction at 2.5 μM concentration. | Signal Transduct Target Ther. 2022 Oct 27;7(1):371. |
| BMDM cells | BMDM cells | 12 h | Acetylshikonin down-regulated the production of IL-6 in a dose-dependent manner, with significant reduction at 2.5 μM concentration. | Signal Transduct Target Ther. 2022 Oct 27;7(1):371. |
| RAW264.7 cells | RAW264.7 cells | 12 h | Acetylshikonin down-regulated the production of IL-6 in a dose-dependent manner, with significant reduction at 2.5 μM concentration. | Signal Transduct Target Ther. 2022 Oct 27;7(1):371. |
| MEF cells and MEF Nur77−/− cells | MEF cells and MEF Nur77−/− cells | 24 h | SK07 induced apoptosis in MEF cells, but its effect was significantly reduced in Nur77 knockout cells. | Cancer Res. 2008 Nov 1;68(21):8871-80. |
| HeLa cervical cancer cells | HeLa cervical cancer cells | 12 or 24 h | Acetylshikonin and its analog SK07 significantly increased Nur77 protein levels in HeLa cells. | Cancer Res. 2008 Nov 1;68(21):8871-80. |
| NIH-H460 lung cancer cells | NIH-H460 lung cancer cells | 12 or 24 h | Acetylshikonin and its analog SK07 significantly increased Nur77 protein levels, while SK06 had a weaker effect. | Cancer Res. 2008 Nov 1;68(21):8871-80. |
| mouse Lewis lung carcinoma cell line LLC | mouse Lewis lung carcinoma cell line LLC | 48 h | Acetylshikonin inhibited the growth of LLC cells in a dose-dependent manner with IC50 of 2.72 ± 0.38 μg/ml. | Chin Med. 2009 Jul 11;4:14. |
| human breast adenocarcinoma cell line MCF-7 | human breast adenocarcinoma cell line MCF-7 | 48 h | Acetylshikonin inhibited the growth of MCF-7 cells in a dose-dependent manner with IC50 of 3.04 ± 0.44 μg/ml. | Chin Med. 2009 Jul 11;4:14. |
| human hepatocellular carcinoma cell line Bel-7402 | human hepatocellular carcinoma cell line Bel-7402 | 48 h | Acetylshikonin inhibited the growth of Bel-7402 cells in a dose-dependent manner with IC50 of 6.82 ± 1.5 μg/ml. | Chin Med. 2009 Jul 11;4:14. |
| human lung adenocarcinoma cell line A549 | human lung adenocarcinoma cell line A549 | 48 h | Acetylshikonin inhibited the growth of A549 cells in a dose-dependent manner with IC50 of 5.6 ± 0.86 μg/ml. | Chin Med. 2009 Jul 11;4:14. |
| Rat neutrophils | Rat neutrophils | 3 min | Acetylshikonin inhibited fMLP/CB-induced superoxide anion generation and oxygen consumption with IC50 values of 0.48 μM and 0.39 μM, respectively. | Br J Pharmacol. 1997 Jun;121(3):409-16. |
| Rat neutrophils | Rat neutrophils | 3 min | Acetylshikonin inhibited PMA-induced superoxide anion generation and oxygen consumption with IC50 values of 0.48 μM and 0.39 μM, respectively. | Br J Pharmacol. 1997 Jun;121(3):409-16. |
| U87 human GBM cells | U87 human GBM cells | 72 h | To evaluate the cytotoxic effects of Acetylshikonin on U87 cells, results showed that all concentrations of ASH induced significant cell death. | Biology (Basel). 2023 Feb 14;12(2):302. |
| U251 human GBM cells | U251 human GBM cells | 72 h | To evaluate the cytotoxic effects of Acetylshikonin on U251 cells, results showed that all concentrations of ASH induced significant cell death. | Biology (Basel). 2023 Feb 14;12(2):302. |
| THP-1 cells | THP-1 cells | 24 h | Acetylshikonin significantly inhibited the proliferation of THP-1 cells. | J Cell Mol Med. 2022 Mar;26(5):1606-1620. |
| K562 cells | K562 cells | 24 h | Acetylshikonin significantly inhibited the proliferation of K562 cells. | J Cell Mol Med. 2022 Mar;26(5):1606-1620. |
| HL-60 cells | HL-60 cells | 24–48 h | Acetylshikonin significantly inhibited the proliferation and viability of HL-60 cells and induced apoptosis through the mitochondrial pathway, while promoting S-phase cell cycle arrest. | J Cell Mol Med. 2022 Mar;26(5):1606-1620. |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice | Ba/F3 EGFR ASV and L861Q allografts model | Oral | 20 and 40 mg/kg | Once daily for 13 days | Evaluate the inhibitory effect of Almonertinib on tumor growth with EGFR ASV and L861Q mutations | Br J Pharmacol. 2020 May;177(10):2303-2319. |
| BALB/c mice | Acute lung injury model | Intragastric administration | 300 mg/kg | Three consecutive days | Acetylshikonin significantly decreased the concentrations of IL-6, TNF-α and IL-1α in BALF and suppressed symptoms of interstitial pneumonia in a concentration-dependent manner. | Signal Transduct Target Ther. 2022 Oct 27;7(1):371. |
| C57BL/6 mice | Lewis lung carcinoma model | Intraperitoneal injection | 0.5, 1, 2 mg/kg | Once every two days, six times in total | Acetylshikonin (2 mg/kg) suppressed LLC tumor growth with an inhibition rate of 42.85%. Immunohistochemical staining showed increased expression of bax and caspase-3 and decreased expression of bcl-2 in acetylshikonin groups. | Chin Med. 2009 Jul 11;4:14. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.03mL 0.61mL 0.30mL |
15.14mL 3.03mL 1.51mL |
30.27mL 6.05mL 3.03mL |
|
| CAS号 | 24502-78-1 |
| 分子式 | C18H18O6 |
| 分子量 | 330.33 |
| SMILES Code | CC(=O)O[C@H](CC=C(C)C)C1=CC(=O)C2=C(C(O)=CC=C2O)C1=O |
| MDL No. | MFCD00143538 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 50 mg/mL(151.36 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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