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  3. Ellagic acid

Ellagic acid  (Synonyms: 鞣花酸)

目录号: HY-B0183 纯度: 99.75%
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Ellagic acid 是一种天然的抗氧化剂,为有效的,ATP 竞争性的 CK2SHP2 抑制剂,IC50Ki 值分别为 40 nM 和 20 nM。

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Ellagic acid

Ellagic acid Chemical Structure

CAS No. : 476-66-4

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Other Forms of Ellagic acid:

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.

IC50 & Target[1]

CK2

40 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Erythrocyte IC50
0.32 mM
Compound: 6
Anticomplement activity in rabbit erythrocytes assessed as concentration required for 50% hemolytic inhibition by alternative pathway pretreated for 10 mins with normal human serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
Anticomplement activity in rabbit erythrocytes assessed as concentration required for 50% hemolytic inhibition by alternative pathway pretreated for 10 mins with normal human serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
[PMID: 29631958]
Erythrocyte IC50
0.32 mM
Compound: 6
Anticomplement activity in sheep erythrocytes assessed as concentration required for 50% hemolytic inhibition by classic pathway pretreated for 10 mins with guinea pig serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
Anticomplement activity in sheep erythrocytes assessed as concentration required for 50% hemolytic inhibition by classic pathway pretreated for 10 mins with guinea pig serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
[PMID: 29631958]
HEK293 IC50
2.93 μM
Compound: EA
Inhibition of catalytic activity of human recombinant FLAG-tagged ppGalNAcT2 W282A mutant expressed in HEK293 cells using EA2 peptide as substrate by HPLC-based enzyme assay
Inhibition of catalytic activity of human recombinant FLAG-tagged ppGalNAcT2 W282A mutant expressed in HEK293 cells using EA2 peptide as substrate by HPLC-based enzyme assay
[PMID: 31227364]
HT-29 EC50
0.11 μM
Compound: Ellagic acid
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 IC50
0.1 μM
Compound: Ellagic acid
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
HUVEC IC50
> 165 μM
Compound: 9
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by fluorescence based assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by fluorescence based assay
[PMID: 37122550]
MDA-MB-231 IC50
27.38 μM
Compound: 4
Cytotoxicity against human MDA-MB-231 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
Cytotoxicity against human MDA-MB-231 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
[PMID: 33359608]
MIA PaCa-2 IC50
149.83 μM
Compound: 4
Cytotoxicity against human MIA PaCa-2 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
Cytotoxicity against human MIA PaCa-2 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
[PMID: 33359608]
Oocyte IC50
270 nM
Compound: ellagic acid
TP_TRANSPORTER: inhibition of ochratoxin A uptake (ochratoxin A / 1uM) in Xenopus laevis oocytes
TP_TRANSPORTER: inhibition of ochratoxin A uptake (ochratoxin A / 1uM) in Xenopus laevis oocytes
[PMID: 15870380]
Panel NCI-60 (60 carcinoma cell lines) GI50
10 nM
Compound: Ellagic acid
Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
[PMID: 15743190]
RAW264.7 IC50
35.7 μM
Compound: 24
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
[PMID: 24679441]
RAW264.7 IC50
> 50 μM
Compound: 12
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by by Griess assay
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by by Griess assay
[PMID: 31419126]
RAW264.7 IC50
> 50 μM
Compound: 24
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
[PMID: 24679441]
SH-SY5Y IC50
300 μM
Compound: EA
Inhibition of beta amyloid in human SH-SY5Y cells
Inhibition of beta amyloid in human SH-SY5Y cells
[PMID: 31563012]
Sf9 IC50
0.25 μM
Compound: EA
Inhibition of human recombinant IGF1R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant IGF1R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.26 μM
Compound: EA
Inhibition of human recombinant TIE2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant TIE2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.34 μM
Compound: EA
Inhibition of human recombinant INS-R expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant INS-R expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.51 μM
Compound: EA
Inhibition of human recombinant ARK5 expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
Inhibition of human recombinant ARK5 expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.58 μM
Compound: EA
Inhibition of human recombinant MET expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant MET expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.69 μM
Compound: EA
Inhibition of human recombinant EGF-R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant EGF-R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.79 μM
Compound: EA
Inhibition of human recombinant VEGF-R2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant VEGF-R2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
0.8 μM
Compound: EA
Inhibition of human recombinant SRC expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant SRC expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
1.09 μM
Compound: EA
Inhibition of human recombinant CDK4/CyclinD1 expressed in Sf9 cells using RB-CTF as substrate after 80 mins by scintillation counting
Inhibition of human recombinant CDK4/CyclinD1 expressed in Sf9 cells using RB-CTF as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
1.3 μM
Compound: EA
Inhibition of human recombinant PDGFRbeta expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant PDGFRbeta expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
1.54 μM
Compound: EA
Inhibition of human recombinant VEGF-R3 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant VEGF-R3 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
1.76 μM
Compound: EA
Inhibition of human recombinant B-RAF expressed in Sf9 cells using MEK1 KM as substrate after 80 mins by scintillation counting
Inhibition of human recombinant B-RAF expressed in Sf9 cells using MEK1 KM as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
1.83 μM
Compound: EA
Inhibition of human recombinant EPHB4 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant EPHB4 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
2.37 μM
Compound: EA
Inhibition of human recombinant COT expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
Inhibition of human recombinant COT expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
2.48 μM
Compound: EA
Inhibition of human recombinant aurora-A expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
Inhibition of human recombinant aurora-A expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
2.5 μM
Compound: EA
Inhibition of human recombinant aurora-B expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
Inhibition of human recombinant aurora-B expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
2.97 μM
Compound: EA
Inhibition of human recombinant SAK expressed in Sf9 cells using p38alpha-KRKR as substrate after 80 mins by scintillation counting
Inhibition of human recombinant SAK expressed in Sf9 cells using p38alpha-KRKR as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
3.11 μM
Compound: EA
Inhibition of human recombinant FAK expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant FAK expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
3.34 μM
Compound: EA
Inhibition of human recombinant AKT1 expressed in Sf9 cells using GSK3(14-27) as substrate after 80 mins by scintillation counting
Inhibition of human recombinant AKT1 expressed in Sf9 cells using GSK3(14-27) as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
3.34 μM
Compound: EA
Inhibition of human recombinant PLK1 expressed in Sf9 cells using casein as substrate after 80 mins by scintillation counting
Inhibition of human recombinant PLK1 expressed in Sf9 cells using casein as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
3.39 μM
Compound: EA
Inhibition of human recombinant CDK2/CyclinA expressed in Sf9 cells using histone H1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant CDK2/CyclinA expressed in Sf9 cells using histone H1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
Sf9 IC50
3.54 μM
Compound: EA
Inhibition of human recombinant ERBB2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
Inhibition of human recombinant ERBB2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
[PMID: 22377675]
U2OS EC50
2.96 μM
Compound: Ellagic acid
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
体外研究
(In Vitro)

Ellagic acid 是一种强效 CK2 抑制剂,IC50 为 40 nM,Ki 为 20 nM,还可阻断其他激酶如 LYN、PKA、SYK、GSK3 等,其 IC50 分别为 2.9、3.5、4.3 和 7.5 μM。Ellagic acid (5-100 μM) 对 Karpas299、SUDHL1、SR786 和 FE-PD 细胞系表现出抑制作用[1]

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

体内研究
(In Vivo)

Ellagic acid (EA;10 mg/kg/天;口服,14 天) 可显著降低大鼠脑中 MDA 含量 17%,并使脑中 TNF-α 水平降低 42%。Ellagic acid 可显著增加 5-HT (39%)、多巴胺 (DA,71%) 和去甲肾上腺素 (NE,77%) 的脑含量。Ellagic acid (10 mg/kg,口服,14 天) 可减轻大鼠中阿霉素引起的组织病理学变化[2]

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

分子量

302.19

Formula

C14H6O8

CAS 号
性状

固体

颜色

Light yellow to khaki

中文名称

鞣花酸

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 2.5 mg/mL (8.27 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3092 mL 16.5459 mL 33.0918 mL
5 mM 0.6618 mL 3.3092 mL 6.6184 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 40 mg/mL (132.37 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.75%

参考文献
Kinase Assay
[1]

CK2 and CK1 phosphorylation assays are carried out at 37°C in the presence of increasing amounts of each inhibitor (Ellagic acid) in a final volume of 25 µL containing 50 mM, Tris-HCl pH 7.5, 100 mM NaCl, 12 mM MgCl2, 0.02 mM [33P-ATP] (500-1000 cpm/pmol), unless otherwise indicated. The phosphorylatable substrates are the synthetic peptide substrate RRRADDSDDDDD (100 µM) and RRKHAAIGDDDDAYSITA (200 µM) for CK2 and CK1, respectively. Reaction started with the addition of the kinase and is stopped after 10 min. by addition of 5 µL of 0.5 M orthophosphoric acid before spotting aliquots onto phosphocellulose filters. Filters are washed in 75 mM phosphoric acid substrate following SDS-PAGE of the radiolabeled samples. DYRK1A, assayed on the peptide RRRFRPASPLRGPPK, and tyrosine kinase activities are determined[1].

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

Cell Assay
[1]

ALCL cell viability is measured by MTT assay. Briefly, 0.1 × 105 cells are seeded onto 96-well microculture plates 12 hrs before adding ellagic acid. The cells are grown in 200 µL of complete RPMI-1640 medium, under standard tissue-culture conditions, in the presence or absence of the drug (Ellagic acid) for 48 hours. Twenty µL of MTT solution (5 mg/mL) are then added to the cell suspension for 4h. The intracellular formazan crystals are dissolved with 150 µL of DMSO and optical density, measured on a spectrophotometer at 540 nm, represents the mean (± SD) of triplicate cultures[1].

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

Animal Administration
[2]

Fifty male adult Sprague-Dawley rats are divided randomly into five groups as follow: Group (1) receives corn oil orally as a vehicle and served as normal control. Group (2) receives doxorubicin (DOX) injection (5 mg/kg, i.p.) twice a week for 14 days. Group (3) receives Ellagic acid (10 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.) twice a week for 14 days. Group (4) receives rosmarinic acid (RA; 75 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.) twice a week for 14 days. Group (5) receives Ellagic acid (10 mg/kg, p.o.; daily) with RA (75 mg/kg, p.o.; daily) for 14 days and DOX injection (5 mg/kg, i.p.) twice a week for 14 days[2].

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3092 mL 16.5459 mL 33.0918 mL 82.7294 mL
5 mM 0.6618 mL 3.3092 mL 6.6184 mL 16.5459 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ellagic acid
目录号:
HY-B0183
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