大黄素 /Emodin
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货号：A178654
同义名：
Frangula emodin;Archin
Emodin（一种蒽醌衍生物）是一种抗SARS-CoV 化合物，阻断SARS冠状病毒 刺突蛋白 与血管紧张素转换酶2（AC E蛋白 激酶2（CK2 ），具有抗炎 和抗癌作用，也是11β-HSD 1的有效选择性抑制剂，对人和鼠11β-HSD 1的IC50 值分别为186 nM和86 nM，在饮食诱导肥胖小鼠中改善代谢紊乱。
Emodin 3D分子结构
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会员价
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Emodin 纯度/质量文件 产品仅供科研
货号：A178654
标准纯度：
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产品说明书
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Emodin 质控信息
PF-670462 2HCl
++++
CK1ε, IC50: 90 nM
CK1δ, IC50: 13 nM
99%+
D4476
++
CK1 from Schizosaccharomyces pombe, IC50: 200 nM
CK1δ, IC50: 300 nM
98%
SR-3029
+++
CK1ε, IC50: 260 nM
CK1δ, IC50: 44 nM
99%+
IWP-2
+++
Wnt
98%
LY364947
++
98%
TA-01
++++
CK1ε, IC50: 6.4 nM
CK1δ, IC50: 6.8 nM
p38 MAPK
99%+
IC261
+
98%
PF-4800567
+++
casein kinase 1 delta, IC50: 711 nM
casein kinase 1 epsilon, IC50: 32 nM
99%+
CK1-IN-1
++++
CK1ε, IC50: 16 nM
CK1δ, IC50: 15 nM
98%
Longdaysin
+
CKIα, IC50: 5.6 μM
CKIδ, IC50: 8.8 μM
99%+
Silmitasertib
++++
99%+
Ellagic acid (hydrate)
+++
PKA
95+%
DMAT
+++
98%
Hematein
++
98+%
Silmitasertib sodium salt
++++
CK2α, IC50: 1 nM
CK2α', IC50: 1 nM
99%+
LY294002
+++
99%+
A-3 HCl
+
++
MLCK,PKA,PKC
98+%
TBB
+
++
98%
TTP 22
++
98%+
DRB
✔
99%+
BioE-1115
+
99%+
(E/Z)-GO289
++++
99%+
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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。
Emodin 生物活性
靶点
描述
Among various Ser/Thr protein kinases, CKII plays a potential role in the processes of cell proliferation, transformation, and differentiation. In addition, abolition of CKII activity causes cell death in yeast, whereas overexpression of the CKII α-subunit gene in animal cells causes the cells to become oncogenic. Emodin, an anthraquinone derivative, selectively and competitively inhibits CKII with IC50 of 2 μM and Ki of 7.2 μM[5] [6] in vivo [7]
Emodin 动物研究
Dose
Nude mice: 10 mg/kg - 80 mg/kg[1] [2] [3]
Administration
i.p., i.v., p.o.
Pharmacokinetics
Animal
Rats[4]
Dose
34.65 mg/kg
Administration
p.o.
V/F
1052 ± 119.8 L
T1/2
23.13 ± 3.56 h
Tmax
0.75 ± 0.00 h
Cmax
91.65 ± 16.82 ng/ml
AUC0→∞
1108 ± 191.1 ng·h/ml
MRT0→∞
29.90 ± 4.71 h
CL/F
31.99 ± 5.15 L/h
AUC0→t
624.7 ± 73.35 ng·h/ml
Emodin 参考文献
[1] Feng Y, Huang SL, et al, Leng Y. Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice. Br J Pharmacol. 2010 Sep;161(1):113-26.
[2] Yim H, Lee YH, et al. Emodin, an anthraquinone derivative isolated from the rhizomes of Rheum palmatum, selectively inhibits the activity of casein kinase II as a competitive inhibitor. Planta Med. 1999 Feb;65(1):9-13.
[3] Liu JX, Zhang JH, et al. Emodin induces Panc-1 cell apoptosis via declining the mitochondrial membrane potential. Oncol Rep. 2012 Dec;28(6):1991-6.
[4] Song P, Kim JH, et al. Emodin regulates glucose utilization by activating AMP-activated protein kinase. J Biol Chem. 2013 Feb 22;288(8):5732-42.
[5] Tzeng TF, Lu HJ, et al. Emodin, a Naturally Occurring Anthraquinone Derivative, Ameliorates Dyslipidemia by Activating AMP-Activated Protein Kinase in High-Fat-Diet-Fed Rats. Evid Based Complement Alternat Med. 2012;2012:781812.
[6] Li RR, Liu XF, et al. Pharmacodynamics of Five Anthraquinones (Aloe-emodin, Emodin, Rhein, Chysophanol, and Physcion) and Reciprocal Pharmacokinetic Interaction in Rats with Cerebral Ischemia. Molecules. 2019 May 17;24(10). pii: E1898.
[7] Yim H, Lee YH, Lee CH, Lee SK. Emodin, an anthraquinone derivative isolated from the rhizomes of Rheum palmatum, selectively inhibits the activity of casein kinase II as a competitive inhibitor. Planta Med. 1999 Feb;65(1):9-13. doi: 10.1055/s-1999-13953. PMID: 10083837.
[8] Xing JY, Song GP, Deng JP, Jiang LZ, Xiong P, Yang BJ, Liu SS. Antitumor Effects and Mechanism of Novel Emodin Rhamnoside Derivatives against Human Cancer Cells In Vitro. PLoS One. 2015 Dec 18;10(12):e0144781. doi: 10.1371/journal.pone.0144781. PMID: 26682731; PMCID: PMC4684281.
[9] Li X, Wang H, Wang J, Chen Y, Yin X, Shi G, Li H, Hu Z, Liang X. Emodin enhances cisplatin-induced cytotoxicity in human bladder cancer cells through ROS elevation and MRP1 downregulation. BMC Cancer. 2016 Aug 2;16:578. doi: 10.1186/s12885-016-2640-3. PMID: 27485374; PMCID: PMC4971704.
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Emodin 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.70mL
0.74mL
0.37mL
18.50mL
3.70mL
1.85mL
37.00mL
7.40mL
3.70mL
Emodin 技术信息
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