货号:A119193
同义名:
麦角甾苷;毛蕊花苷
/ Kusaginin; TJC160
Acteoside是从Cistanche deserticola Y.C. Ma植物中分离提取的天然产物,具有抗氧化作用,且为PKC抑制剂(IC50 = 25 μM)。


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| 产品名称 | PKC ↓ ↑ | PKCα ↓ ↑ | PKCβ ↓ ↑ | PKCγ ↓ ↑ | PKCδ ↓ ↑ | PKCε ↓ ↑ | PKCζ ↓ ↑ | PKCη ↓ ↑ | PKCθ ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Daphnetin |
+
PKC, IC50: 25.01 μM |
EGFR,PKA | 95% | ||||||||||||||||
| Dequalinium Chloride | 99%+ | ||||||||||||||||||
| Quercetin | ✔ | Sirtuin,Src | 95% | ||||||||||||||||
| Myricetrin | ✔ | 96% | |||||||||||||||||
| Go 6983 |
+++
PKCα, IC50: 7 nM |
+++
PKCβ, IC50: 7 nM |
+++
PKCγ, IC50: 6 nM |
+++
PKCδ, IC50: 10 nM |
++
PKCζ, IC50: 60 nM |
99%+ | |||||||||||||
| Go6976 |
+++
PKC, IC50: 7.9 nM |
++++
PKCα, IC50: 2.3 nM |
+++
PKCβ1, IC50: 6.2 nM |
FLT3 | 99%+ | ||||||||||||||
| Bisindolylmaleimide I |
+++
PKCα, IC50: 20 nM |
+++
PKCβ2, IC50: 16 nM PKCβ1, IC50: 17 nM |
+++
PKCγ, IC50: 20 nM |
99%+ | |||||||||||||||
| Lawsone methyl ether | ✔ | 99% | |||||||||||||||||
| Sotrastaurin |
++++
PKCα, Ki: 0.95 nM |
++++
PKCβ1, Ki: 0.64 nM |
++++
PKCδ, Ki: 2.1 nM |
++++
PKCε, Ki: 3.2 nM |
++++
PKCη, Ki: 1.8 nM |
++++
PKCθ, Ki: 0.22 nM |
99%+ | ||||||||||||
| Enzastaurin |
++
PKCα, IC50: 39 nM |
+++
PKCβ, IC50: 6 nM |
+
PKCγ, IC50: 83 nM |
+
PKCε, IC50: 110 nM |
98% | ||||||||||||||
| Midostaurin |
++
PKCα, IC50: 22 nM |
++
PKCβ2, IC50: 31 nM PKCβ1, IC50: 30 nM |
++
PKCγ, IC50: 24 nM |
+
PKCδ, IC50: 330 nM |
+
PKCε, IC50: 1.25 μM |
+
PKCη, IC50: 160 nM |
99% | ||||||||||||
| Ro 31-8220 mesylate |
++++
PKCα, IC50: 5 nM |
+++
PKCβ2, IC50: 14 nM PKCβ1, IC50: 24 nM |
++
PKCγ, IC50: 27 nM |
++
PKCε, IC50: 24 nM |
99%+ | ||||||||||||||
| Staurosporine |
++++
PKCα, IC50: 2 nM |
++++
PKCγ, IC50: 5 nM |
+++
PKCδ, IC50: 20 nM |
++
PKCε, IC50: 73 nM |
++++
PKCη, IC50: 4 nM |
99%+ | |||||||||||||
| Ruboxistaurin HCl |
+
PKCα, IC50: 0.36 μM |
++++
PKCβ2, IC50: 5.9 nM PKCβ1, IC50: 4.7 nM |
+
PKCγ, IC50: 0.3 μM |
+
PKCδ, IC50: 0.25 μM |
++
PKCη, IC50: 0.052 μM |
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。 | |||||||||||||||||||
| 产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
| LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
| ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
| K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
| LDN-193189 2HCl |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
| LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
| DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
| SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
| Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
| Alantolactone | ✔ | 98% | |||||||||||||||||
| (E/Z)-SIS3 free base | ✔ | 97% | |||||||||||||||||
| Pirfenidone | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
| GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
| LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
| SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
| SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
| LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
| Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
| SB 431542 |
+
ALK5, IC50: 94 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 | Acteoside (Verbascoside) is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity[3]. Acteoside inhibited cell proliferation, colony formation and migration in all the three human HCC cell lines BEL7404, HLF and JHH-7. The prohibition of angiogenesis by acteoside was revealed by the inhibition of tube formation and cell migration of HUVECs[4]. ACT (Acteoside) has the potential therapeutic effect on OA (Osteoarthritis) through inhibiting the inflammatory responses via inactivating JAK/STAT signaling pathway[5]. Acteoside can alleviate mesangial cell inflammatory injury by modulating Th22 lymphocytes chemotaxis and proliferation[6]. In addition, acteoside could penetrate BBB (blood-brain-barrier) and have potential therapeutic value for PD (Parkinson's disease) by activating the Nrf2/ARE signaling pathway and attenuating the oxidative stress[7]. |
| Concentration | Treated Time | Description | References | |
| C5N cells | 500 μM | 24 h | Acteoside showed lower toxicity in C5N cells but increased cellular ROS levels. | Redox Biol. 2018 Jun;16:169-178 |
| A5 cells | 500 μM | 24 h | Acteoside showed increased toxicity in A5 cells, elevated cellular ROS levels, and suppressed MMP-2 and MMP-9 enzymatic activities. | Redox Biol. 2018 Jun;16:169-178 |
| RAW 264.7 cell line | 50 µM | 24 h | Evaluate the inhibitory effect of Acteoside on macrophage activation, showing significant inhibition of IL-6 secretion at 50 μmol/L. | Engineering (Beijing). 2023 Jan;20:63-76. |
| Hepatocytes (BRL-3A) | 25, 50, 100 μM | 16 h | To investigate the effect of Acteoside on HR-induced hepatocyte injury. Results showed that Acteoside reduced the release of injury markers (e.g., HMGB1) from hepatocytes under HR conditions. | Int J Biol Sci. 2023 Sep 18;19(15):4967-4988 |
| Liver sinusoidal endothelial cells (LSECs) | 25, 50, 100 μM | 12 h | To evaluate the effect of Acteoside on hypoxia-reoxygenation (HR)-induced senescent phenotype in LSECs. Results showed that Acteoside significantly inhibited the upregulation of senescence markers (e.g., p21, p53) and restored the expression of cell cycle checkpoints (e.g., cdk2, ccnd1). | Int J Biol Sci. 2023 Sep 18;19(15):4967-4988 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Hepatic ischemia-reperfusion injury (HIRI) model | Oral gavage | 25, 50, 100 mg/kg | Once daily for 7 days | To evaluate the protective effect of Acteoside on liver injury in HIRI mice. Results showed that Acteoside significantly ameliorated HIRI-induced liver histopathological injury, abnormal liver function indicators, and senescent phenotype of LSECs. | Int J Biol Sci. 2023 Sep 18;19(15):4967-4988 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03641248 | Osteoarthritis, Knee | Early Phase 1 | Not yet recruiting | June 2019 | United States, Missouri ... 展开 >> Univ of Missouri Health Care Center Not yet recruiting Columbia, Missouri, United States, 65211 Contact: Dean Hainsworth, MD 573-882-4894 ClinicalResearch@health.missouri.edu 收起 << |
| NCT02662283 | IGA Nephropathy | Phase 2 Phase 3 | Unknown | November 2016 | China, Guangdong ... 展开 >> Department of Nephrology, 6th Affiliated Hospital, Sun Yat-Sen University Guangzhou, Guangdong, China, 510655 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.60mL 0.32mL 0.16mL |
8.01mL 1.60mL 0.80mL |
16.01mL 3.20mL 1.60mL |
|
| CAS号 | 61276-17-3 |
| 分子式 | C29H36O15 |
| 分子量 | 624.59 |
| SMILES Code | O=C(O[C@@H]1[C@@H](CO)O[C@@H](OCCC2=CC=C(O)C(O)=C2)[C@H](O)[C@H]1O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](O)[C@H]3O)/C=C/C4=CC=C(O)C(O)=C4 |
| MDL No. | MFCD00221751 |
| 别名 | 麦角甾苷;毛蕊花苷;毛蕊花糖苷 ;Kusaginin; TJC160; Acetoside; NSC 603831; Verbascoside |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, room temperature |
| 溶解方案 |
DMSO: 105 mg/mL(168.11 mM),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 H2O: 100 mg/mL(160.11 mM) 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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