同义名 :	金诺芬 ;SKF-39162; NSC 321521; NSC 321521, Ridauragold thiol; Ridaura; SKF-D-39162; Ridauragold thiol
	CAS号 :	34031-32-8
	货号 :	A361974
	分子式 :	C20H34AuO9PS
	纯度 :	99%+
	分子量 :	678.48
	MDL号 :	MFCD00080759
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	Deubiquitinases (DUBs) are proteases that cleave ubiquitin or ubiquitin-like proteins from ubiquitin pro-proteins or conjugates with target proteins and they are responsible for maintenance of protein homeostasis in cells. Increased proteasome activity has been reported in many different cancers, such as colon and prostate cancers and leukemia, than in non-cancer cells, suggesting that DUBs are becoming attractive targets of cancer therapy. Auranofin inhibits proteasome-associated DUBs UCHL5 and USP14 rather than the 20S proteasome which is required for Auranofin-induced cytotoxicity. Auranofin reduced the cell viability via caspase activation in a dose-dependent manner with the IC50 values of 0.43 (24 h) and 0.17 μM (48 h) in HepG2 cells and 1.5 (24 h) and 0.41 μM (48 h) in MCF-7 cells, respectively[3]. Rats subjected to left ventricular hypertrophy via abdominal aorta constriction (AAC) showed enhanced chamber diameters and left ventricular function and decreased ejection fraction and fractional shortening values after intraperitoneal injections of 3 mg/kg Auranofin daily for 8 weeks, compared with AAC rats. Also, Auranofin treatment decreased proteasome activity and inactivation of the NF-κB signaling pathway in cardiac tissue[4]. Auranofin also shows potent bactericidal activities against M. tuberculosis, Bacillus subtilis, Enterococcus faecalis, Enterococcus faecium and Staphylococcus aureus[5].
作用机制	Auranofin inhibits 26S proteasome-associated DUBs UCHL5 and USP14 by targeting 19S RP.

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
NCT01557348	-		Completed	-	-
NCT02770378	Glioblastoma	Phase 1	Active, not recruiting	March 2020	Germany ... 展开 >> University of Ulm School of Medicine Ulm, Baden-Württemberg, Germany, 89081 收起 <<
NCT01557348	-		Completed	-	-

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.47mL 0.29mL 0.15mL	7.37mL 1.47mL 0.74mL	14.74mL 2.95mL 1.47mL

参考文献

[1]Liu N, Li X, et al. Clinically used antirheumatic agent auranofin is a proteasomal deubiquitinase inhibitor and inhibits tumor growth. Oncotarget. 2014;5(14):5453-71 [2]Hu M, Zhang Z, et al. Deubiquitinase Inhibitor Auranofin Attenuated Cardiac Hypertrophy by Blocking NF-κB Activation. Cell Physiol Biochem. 2018;45(6):2421-2430 [3]Liu N, Li X, Huang H, Zhao C, Liao S, Yang C, Liu S, Song W, Lu X, Lan X, Chen X, Yi S, Xu L, Jiang L, Zhao C, Dong X, Zhou P, Li S, Wang S, Shi X, Dou PQ, Wang X, Liu J. Clinically used antirheumatic agent auranofin is a proteasomal deubiquitinase inhibitor and inhibits tumor growth. Oncotarget. 2014 Jul 30;5(14):5453-71. doi: 10.18632/oncotarget.2113. PMID: 24977961; PMCID: PMC4170648. [4]Hu M, Zhang Z, Liu B, Zhang S, Chai R, Chen X, Kong T, Zhang F, Zhang J, Liu S, Liu N. Deubiquitinase Inhibitor Auranofin Attenuated Cardiac Hypertrophy by Blocking NF-κB Activation. Cell Physiol Biochem. 2018;45(6):2421-2430. doi: 10.1159/000488230. Epub 2018 Mar 15. PMID: 29554646. [5]Harbut MB, Vilchèze C, Luo X, Hensler ME, Guo H, Yang B, Chatterjee AK, Nizet V, Jacobs WR Jr, Schultz PG, Wang F. Auranofin exerts broad-spectrum bactericidal activities by targeting thiol-redox homeostasis. Proc Natl Acad Sci U S A. 2015 Apr 7;112(14):4453-8. doi: 10.1073/pnas.1504022112. Epub 2015 Mar 23. PMID: 25831516; PMCID: PMC4394260.