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Embelin

现货
Catalog No.
A8235
细胞通透的XIAP抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 500.00
现货
50mg
¥ 1,900.00
Ship with 10-15 days

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Background

Embelin, a natural benzoquinone from plants of the genus Embelia, is an inhibitor of X-linked inhibitor of apoptosis protein (XIAP) with IC50 of 4.1 μM.
XIAP is a member of the inhibitor of apoptosis family of proteins. This protein modulates signaling pathways involved in cell apoptosis and stops cell apoptosis induced by viral infection or overproduction of caspases.
Embelin was shown to exhibit anti-tumor and anti-inflammatory activity in cells. For instance, embelin inhibits cell growth and activates caspases to promote apoptosis in cancer cells with high expression of XIAP [1]. Additionally, embelin was reported to prevent NF-κB activation by inhibiting IKK and thus resulted in suppression of NF-κB-regulated anti-apoptotic and metastatic gene expression [2].
Embelin has also been used extensively in various animal models to study the role of XIAP. In the azoxymethane/dextran sulfate sodium (AOM/DSS) induced colitis-associated cancer (CAC) model, embelin reduced both incidence and tumor size in mice by inhibiting proliferation of tumor epithelial cells and suppressing IL6 expression and IL6-activated STAT3 in vivo [3].
References
1.Nikolovska-Coleska Z, Xu L, Hu Z, Tomita Y, Li P, Roller PP, et al. Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database. J Med Chem 2004,47:2430-2440.
2.Ahn KS, Sethi G, Aggarwal BB. Embelin, an inhibitor of X chromosome-linked inhibitor-of-apoptosis protein, blocks nuclear factor-kappaB (NF-kappaB) signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Mol Pharmacol 2007,71:209-219.
3.Dai Y, Jiao H, Teng G, Wang W, Zhang R, Wang Y, et al. Embelin reduces colitis-associated tumorigenesis through limiting IL-6/STAT3 signaling. Mol Cancer Ther 2014,13:1206-1216.

Chemical Properties

Physical AppearanceA solid
StorageStore at 4°C
M.Wt294.39
Cas No.550-24-3
FormulaC17H26O4
Solubility≥9.6mg/mL in DMSO, ≥4.23 mg/mL in EtOH with ultrasonic, <2.15 mg/mL in H2O
Chemical Name2,5-dihydroxy-3-undecylcyclohexa-2,5-diene-1,4-dione
SDFDownload SDF
Canonical SMILESCCCCCCCCCCCC1=C(C(=O)C=C(C1=O)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

荧光偏振竞争性结合测定

在黑色、圆底的Dynex 96孔板上进行荧光偏振实验。将5 μL Embelin稀释液(溶剂为DMSO),预孵育的XIAP BIR3蛋白 (0.06 μM) 以及Smac肽 (SM7F) N末端 (0.01 μM) 加入到测定缓冲液中,最终体积为125 μL。每个实验包含:含XIAP BIR3蛋白和SM7F(相当于0%抑制)的结合肽,以及对照,仅含游离SM7F(相当于100%抑制)的游离肽对照物。将反应物混合,将其置于室温下孵育3小时以达到平衡。

细胞实验 [1]:

细胞系

PC-3、LNCap、PrEC和WI-38细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

1 ~ 64 μM;4 ~ 5天

实验结果

Embelin呈剂量依赖性地抑制PC-3细胞和LNCaP细胞生长,其IC50值分别为3.7 μM和5.7 μM。在正常的PrEC和WI-38细胞中,Embelin毒性相对较低,其IC50值分别为20.1 μM和19.3 μM。

动物实验 [2]:

动物模型

AOM/DSS诱导的结肠炎相关癌症 (CAC) 模型

给药剂量

50 mg/kg/day;口服给药

实验结果

在CAC小鼠模型中,Embelin抑制肿瘤上皮细胞增殖以及IL-6表达和IL6活化STAT3,从而减少肿瘤发生和肿瘤大小。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Nikolovska-Coleska Z, Xu L, Hu Z, Tomita Y, Li P, Roller PP, et al. Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database. J Med Chem 2004,47:2430-2440.

[2]. Dai Y, Jiao H, Teng G, Wang W, Zhang R, Wang Y, et al. Embelin reduces colitis-associated tumorigenesis through limiting IL-6/STAT3 signaling. Mol Cancer Ther 2014,13:1206-1216.

生物活性

描述 Embelin是XIAP抑制剂,IC50值4.1 μM。
靶点 5-LO mPGES-1 XIAP      
IC50 0.06 μM 0.2 μM 4.1 μM      

质量控制

质量控制和MSDS

批次:

化学结构

Embelin