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Damnacanthal
目录号: PC16150 纯度: ≥98%
CAS No. :477-84-9
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中文名称
Damnacanthal
中文别名
丹宁卡;[5-氟-2-甲基-3-(喹啉-2-基甲基)吲哚-1-基]乙酸;3-羟基-1-甲氧基-2-蒽醌甲醛;丹拿堪索
英文名称
Damnacanthal
英文别名
Damnacanthal;2-Anthracenecarboxaldehyde,9,10-dihydro-3-hydroxy-1-methoxy-9,10-dioxo-;DAMNACANTHAL(RG);3-hydroxy-1-methoxy-9,10-dioxoanthracene-2-carbaldehyde;3-Hydroxy-1-methoxy-2-anthraquinonecarboxaldehyde;[ "" ]
Cas No.
477-84-9
分子式
C16H10O5
分子量
282.25
包装储存

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 tyrosine kinase activity. Natural Damnacanthal inhibits p56 autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.

性状

Solid

IC50 & Target[1][2]

IC50: 46 nM (p56 autophosphorylation) and 220 nM (phosphorylation of exogenous substrates by p56 );
Apoptosis;
Candida albicans

体外研究(In Vitro)

Damnacanthal has > 100-fold selectivity for p56 over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56 over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56 over the homologous enzymes p60 and p59.
Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner.
Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.
Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis.
Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced.
Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner.

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

Cell Proliferation Assay

Cell Line: HCT-116 and SW480 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 1, 2, and 4 days
Result: Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner.

Cell Cycle Analysis

Cell Line: HCT-116 cells
Concentration: 1 μM, 10 μM and 50 μM
Incubation Time: 72 hours
Result: Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.

Apoptosis Analysis

Cell Line: HCT-116 cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Significantly increased caspase 3/7 activity.

Western Blot Analysis

Cell Line: HCT-116 cells
Concentration: 0.1 μM, 1 μM and 10 μM
Incubation Time: 24 hours
Result: NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM.
体内研究(In Vivo)

Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema.

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

Animal Model: Male ddY mice (5-6 weeks) injected with formalin or Histamine
Dosage: 10 mg/kg, 30 mg/kg and 100 mg/kg
Administration: Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result: Significantly reduced the growth of human lung tumor without acute toxicity.
运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

结构分类
来源
参考文献
溶解度数据
体外研究: 

DMSO : 5 mg/mL (17.71 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5430 mL 17.7148 mL 35.4296 mL
5 mM 0.7086 mL 3.5430 mL 7.0859 mL
10 mM 0.3543 mL 1.7715 mL 3.5430 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    建议依照次序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 4 mg/mL (14.17 mM); Suspended solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 4 mg/mL (14.17 mM); Suspended solution; Need ultrasonic

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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