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                同义名:
                    
                        
                            白术内酯II
                            
                             / Asterolide; 2-Atractylenolide
                            
                        
                    
                
                
                
                    
                     
                
            
Atractylenolide II是从白术干燥根茎中分离的倍半萜化合物,具有抗增殖、抗黑色素瘤、改善心肌纤维化和神经保护等活性。它通过抑制 STAT3 信号通路来发挥抗黑色素瘤作用。
 
                                 
                                
                            

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| 产品名称 | Cdc ↓ ↑ | CDK1 ↓ ↑ | CDK19 ↓ ↑ | CDK2 ↓ ↑ | CDK3 ↓ ↑ | CDK4 ↓ ↑ | CDK5 ↓ ↑ | CDK6 ↓ ↑ | CDK7 ↓ ↑ | CDK8 ↓ ↑ | CDK9 ↓ ↑ | CLK ↓ ↑ | 其他靶点 | 纯度 | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| XL413 HCl | ++++ Cdc7, IC50: 3.4 nM | 99%+ | |||||||||||||||||
| SU9516 | +++ CDK1, IC50: 40 nM | +++ CDK2, IC50: 22 nM | ++ CDK4, IC50: 200 nM | 99%+ | |||||||||||||||
| RO-3306 | +++ CDK1, Ki: 20 nM | ERK,SGK | 98% | ||||||||||||||||
| R547 | ++++ CDK1/CyclinB, Ki: 2 nM | ++++ CDK2/CyclinE, Ki: 3 nM | ++++ CDK4/CyclinD1, Ki: 1 nM | 99%+ | |||||||||||||||
| BMS-265246 | ++++ CDK1/CyclinB, IC50: 6 nM | ++++ CDK2/CyclinE, IC50: 9 nM | + CDK4/CyclinD, IC50: 230 nM | 99%+ | |||||||||||||||
| NU6027 | + CDK1, Ki: 2.5 μM | + CDK2, Ki: 1.3 μM | DNA-PK | 98% | |||||||||||||||
| Purvalanol A | ++++ Cdc2/CyclinB, IC50: 4 nM | +++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM | + CDK4/CyclinD1, IC50: 850 nM | 99%+ | |||||||||||||||
| SCH900776 | ++ CDK2, IC50: 0.16 μM | 99%+ | |||||||||||||||||
| AUZ 454 | ++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM | 99%+ | |||||||||||||||||
| A-674563 HCl | ++ CDK2, Ki: 46 nM | PKA | 99% | ||||||||||||||||
| JNJ-7706621 | ++++ CDK1/CyclinB, IC50: 9 nM | ++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM | ++ CDK3/CyclinE, IC50: 58 nM | + CDK4/CyclinD1, IC50: 253 nM | ++ CDK6/CyclinD1, IC50: 175 nM | 99%+ | |||||||||||||
| AT7519 | ++ CDK1/CyclinB, IC50: 210 nM | ++ CDK2/CyclinA, IC50: 47 nM | + CDK3/CyclinE, IC50: 360 nM | ++ CDK4/CyclinD1, IC50: 100 nM | +++ CDK5/p35, IC50: 13 nM | ++ CDK6/CyclinD3, IC50: 170 nM | ++++ CDK9/CyclinT, IC50: <10 nM | 98+% | |||||||||||
| PHA-793887 | ++ CDK1/CyclinB, IC50: 60 nM | ++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM | ++ CDK4/CyclinD1, IC50: 62 nM | ++++ CDK5/p25, IC50: 5 nM | ++++ CDK7/CyclinH, IC50: 10 nM | ++ CDK9/CyclinT1, IC50: 138 nM | 99%+ | ||||||||||||
| Milciclib | + CDK1/CyclinB, IC50: 398 nM | ++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM | ++ CDK4/CyclinD1, IC50: 160 nM | + CDK5/p35, IC50: 265 nM | ++ CDK7/CyclinH, IC50: 150 nM | 99%+ | |||||||||||||
| Kenpaullone | + CDK1/CyclinB, IC50: 0.4μM | + CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM | + CDK5/p35, IC50: 0.85μM | 98% | |||||||||||||||
| SNS-032 | +++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM | + CDK5/p35, IC50: 340 nM | ++ CDK7/CyclinH, IC50: 62 nM | ++++ CDK9/CyclinT, IC50: 4 nM | 99%+ | ||||||||||||||
| Dinaciclib | ++++ CDK1, IC50: 3 nM | ++++ CDK2, IC50: 1 nM | ++++ CDK5, IC50: 1 nM | ++++ CDK9, IC50: 4 nM | 99%+ | ||||||||||||||
| PHA-767491 HCl | ++++ Cdc7, IC50: 10 nM | + CDK1, IC50: 250 nM | + CDK2, IC50: 240 nM | + CDK5, IC50: 460 nM | +++ CDK9, IC50: 34 nM | MK2 | 99% | ||||||||||||
| (R)-Roscovitine | + Cdc2/CyclinB, IC50: 0.65 μM | + CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM | ++ CDK5/p35, IC50: 0.16 μM | 99%+ | |||||||||||||||
| Narazaciclib | ++++ CDK4/CyclinD1, IC50: 3.87 nM | ++++ CDK6/CyclinD1, IC50: 9.82 nM | RET | 99%+ | |||||||||||||||
| Palbociclib | ++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM | +++ CDK6/CyclinD2, IC50: 15 nM | 99% | ||||||||||||||||
| Abemaciclib | ++++ CDK4, IC50: 2 nM | ++++ CDK6, IC50: 10 nM | 99% | ||||||||||||||||
| Ribociclib | ++++ CDK4, IC50: 10 nM | +++ CDK6, IC50: 39 nM | 98% | ||||||||||||||||
| Palbociclib isethionate | ++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM | +++ CDK6/CyclinD2, IC50: 15 nM | 99%+ | ||||||||||||||||
| BS-181 HCl | +++ CDK7, IC50: 21 nM | 99%+ | |||||||||||||||||
| (E/Z)-THZ1 2HCl | ++++ CDK7, IC50: 3.2 nM | 99%+ | |||||||||||||||||
| LDC4297 | ++++ CDK7, IC50: 0.13 nM | 99%+ | |||||||||||||||||
| Senexin A | + CDK19, Kd: 0.31 μM | + CDK8, Kd: 0.83 μM | 99% | ||||||||||||||||
| MSC2530818 | ++++ CDK8, IC50: 2.6 nM | 99%+ | |||||||||||||||||
| Wogonin | ✔ | 99%+ | |||||||||||||||||
| Riviciclib HCl | ++ CDK1/CyclinB, IC50: 79 nM | + CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM | ++ CDK4/CyclinD1, IC50: 63 nM | + CDK6/CyclinD3, IC50: 396 nM | + CDK7/CyclinH, IC50: 2.87 μM | +++ CDK9/CyclinT1, IC50: 20 nM | 98% | ||||||||||||
| LDC000067 | + CDK2, IC50: 2.441 μM | ++ CDK9, IC50: 44 nM | 98% | ||||||||||||||||
| Flavopiridol | +++ CDK1, IC50: 40 nM | +++ CDK2, IC50: 40 nM | +++ CDK4, IC50: 40 nM | +++ CDK6, IC50: 40 nM | + CDK7, IC50: 300 nM | +++ CDK9, IC50: 20 nM | 99%+ | ||||||||||||
| LY2857785 | + CDK7, IC50: 0.246 μM | +++ CDK8, IC50: 0.016 μM | +++ CDK9, IC50: 0.011 μM | 99%+ | |||||||||||||||
| AZD-5438 | +++ CDK1, IC50: 16 nM | ++++ CDK2, IC50: 6 nM | +++ CDK9, IC50: 20 nM | 99%+ | |||||||||||||||
| ML167 | ++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM | 99%+ | |||||||||||||||||
| (E/Z)-TG003 | +++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM | 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 | Atractylenolide II is a sesquiterpene compound isolated from the dried rhizome of Atractylodes macrocephala (Baizhu in Chinese) with anti-proliferative activity. | 
| Concentration | Treated Time | Description | References | |
| GES-1 cells | 400 μM | 48 h | no cytotoxicity | Molecules. 2017 Nov 3;22(11):1886 | 
| AGS cells | 400 μM | 48 h | significantly inhibited cell proliferation and induced apoptosis | Molecules. 2017 Nov 3;22(11):1886 | 
| AN3CA cells | 0, 25, 50, 100, 200, 400 µM | 24, 48, 72 h | Inhibited cell proliferation and glycolysis, induced apoptosis | Molecules. 2024 Feb 21;29(5):939 | 
| HCT15 cells | 80 μM | 24 h | AT-II significantly inhibited the growth and migration abilities of HCT15 cells, with enhanced effects when combined with IFN-γ. | J Cancer. 2024 Jun 11;15(13):4328-4344 | 
| HT29 cells | 80 μM | 24 h | AT-II significantly inhibited the growth and migration abilities of HT29 cells, with enhanced effects when combined with IFN-γ. | J Cancer. 2024 Jun 11;15(13):4328-4344 | 
| Lovo cells | 50 μg/mL | 48 h | Atractylenolide II significantly inhibited the proliferation and viability of Lovo cells and enhanced their sensitivity to 5-fluorouracil, mitomycin, adriamycin, and cisplatin. | J Cell Mol Med. 2019 May;23(5):3151-3165 | 
| SW480 cells | 50 μg/mL | 48 h | Atractylenolide II significantly inhibited the proliferation and viability of SW480 cells and enhanced their sensitivity to 5-fluorouracil, mitomycin, adriamycin, and cisplatin. | J Cell Mol Med. 2019 May;23(5):3151-3165 | 
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice and C57BL/6 mice | Colorectal cancer xenograft model and lung metastasis model | Intraperitoneal injection | 50 mg/kg | Once daily for 21 days | AT-II alone or in combination with IFN-γ significantly inhibited tumor growth and lung metastasis, and improved the tumor microenvironment. | J Cancer. 2024 Jun 11;15(13):4328-4344 | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 4.30mL 0.86mL 0.43mL | 21.52mL 4.30mL 2.15mL | 43.04mL 8.61mL 4.30mL | |
| CAS号 | 73069-14-4 | 
| 分子式 | C15H20O2 | 
| 分子量 | 232.32 | 
| SMILES Code | O=C1C(C)=C(C[C@@]23[H])[C@@](C[C@@]3(C)CCCC2=C)([H])O1 | 
| MDL No. | MFCD09037396 | 
| 别名 | 白术内酯II ;Asterolide; 2-Atractylenolide | 
| 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, 2-8°C | 
| 溶解方案 | DMSO: 105 mg/mL(451.97 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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