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Embelin

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Chemical Structure| 550-24-3 同义名 : 恩贝酸/恩贝灵 ;Emberine;NSC 91874;Embelic acid
CAS号 : 550-24-3
货号 : A116360
分子式 : C17H26O4
纯度 : 99%+
分子量 : 294.386
MDL号 : MFCD00016369
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(169.85 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
动物实验配方：
生物活性
靶点

  • XIAP

    XIAP, IC50:4.1 μM
描述 Embelin is a potent XIAP inhibitor with IC50 value of 4.1μM (measured by FP-based biochemical binding assay) [1]. Pretreatment with embelin 12h prior to TNFα at concentration ranging in 10-50μM can dose-dependently inhibit TNFα-induced NF-κB activation by inhibiting IκB degradation, as well as inhibted TNFα-induced p65 nuclear translocation due to inhibition of p65 phosphorylation in KBM-5 cells. with no affect on protein level of IAP1, IAP2 and XIAP. Exposure to 50μM embelin for 6-24h could reduce the antiapoptotic proteins survivin, IAP1/2, and suppress Bcl-xL, cFLIP, and TRAF1, suppress the cell proliferation gene expression, including COX-2, cyclin D1 and c-Myc, as well as gene products involved in tumor metastasis, including VEGF, MMP-9 and ICAM-1, which were all TNF-induced NF-κB-dependent[2]. The induction of autophagic and apoptotic cell death by embelin can also be observed in human oral squamous cell carcinoma Ca9-22 cell line[3]. Neonatal injections of 20mg/kg embelin, s.c., could exacerbate hypoxia-ischemia-induced persistent behavioral deficits in female rats on postnatal day 7, but not in male rats[4].
作用机制 Embelin bind to the XIAP-BIR3 domain where caspase-9 and Smac proteins bind. [1]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02785172 Psoriasis Phase 2 Completed - United States, California ... 展开 >> Valeant Site 12 Fullerton, California, United States, 92831 Valeant Site 04 La Mesa, California, United States, 91941 Valeant Site 03 San Diego, California, United States, 92093 Valeant Site 09 San Diego, California, United States, 92093 United States, Florida Valeant Site 05 Lauderdale Lakes, Florida, United States, 33313 Valeant Site 02 Miami, Florida, United States, 33111 United States, Minnesota Valeant Site 07 Fridley, Minnesota, United States, 55421 United States, North Carolina Valeant Site 08 Chapel Hill, North Carolina, United States, 27514 United States, Ohio Valeant Site 06 Columbus, Ohio, United States, 43085 United States, South Carolina Valeant Site 13 Mount Pleasant, South Carolina, United States, 29464 United States, Texas Valeant Site 11 Katy, Texas, United States, 77449 Valeant Site 10 San Antonio, Texas, United States, 78201 Valeant Site 01 Sugar Land, Texas, United States, 77479 United States, Utah Valeant Site 14 Salt Lake City, Utah, United States, 84103 收起 <<
NCT03058744 Psoriasis Phase 1 Completed - United States, California ... 展开 >> Valeant Site 12 Anaheim, California, United States, 92801 Valeant Site 05 Encino, California, United States, 91436 Valeant Site 01 San Diego, California, United States, 92093 Valeant Site 07 Santa Rosa, California, United States, 95401 United States, Florida Valeant Site 10 Orange Park, Florida, United States, 32065 Valeant Site 09 Sanford, Florida, United States, 32771 United States, Georgia Valeant Site 08 Atlanta, Georgia, United States, 30301 United States, Indiana Valeant Site 04 Plainfield, Indiana, United States, 46168 United States, New York Valeant Site 06 New York, New York, United States, 10001 United States, Pennsylvania Valeant Site 11 Philadelphia, Pennsylvania, United States, 19019 United States, Texas Valeant Site 03 Austin, Texas, United States, 73301 Valeant Site 02 Katy, Texas, United States, 77449 收起 <<
NCT01567215 Fetus or Newborn Affected by C... 展开 >>ondition of Umbilical Cord 收起 << Phase 2 Completed - Denmark ... 展开 >> Hvidovre Hospital Kettegård Alle 31, Hvidovre, Denmark, 2650 Hvidovre University Hospital Hvidovre, Kettegård alle 30, Denmark, 2650 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

16.98mL

3.40mL

1.70mL

33.97mL

6.79mL

3.40mL
参考文献

[1]Nikolovska-Coleska Z, Xu L, 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 May 6;47(10):2430-40.

[2]Ahn KS, Sethi G, et al. 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 Jan;71(1):209-19. Epub 2006 Oct 6.

[3]Lee YJ, Park BS, et al. XIAP inhibitor embelin induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells. Environ Toxicol. 2017 Nov;32(11):2371-2378.

[4]Hill CA, Alexander ML, et al. Inhibition of X-linked inhibitor of apoptosis with embelin differentially affects male versus female behavioral outcome following neonatal hypoxia-ischemia in rats. Dev Neurosci. 2011;33(6):494-504.

[5]Li Z, Chen SJ, et al. Pharmacokinetic and Bioavailability Studies of Embelin after Intravenous and Oral Administration to Rats. Evid Based Complement Alternat Med. 2019 Mar 20;2019:9682495.

[6]Bhuvanendran S, Kumari Y, et al. Amelioration of Cognitive Deficit by Embelin in a Scopolamine-Induced Alzheimer's Disease-Like Condition in a Rat Model. Front Pharmacol. 2018 Jun 25;9:665.