Authors Sun, WN; Chen, XL; Huang, SZ; Li, WP; Tian, CY; Yang, SY; Li, LL in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Sun, Weining; Tian, Chenyu; Li, Linli] Sichuan Univ, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst, Minist Educ, Chengdu 610041, Sichuan, Peoples R China; [Chen, Xiuli; Huang, Shenzhen; Li, Wenpei; Yang, Shengyong] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China; [Chen, Xiuli; Huang, Shenzhen; Li, Wenpei; Yang, Shengyong] Sichuan Univ, West China Hosp, Canc Ctr, Chengdu 610041, Sichuan, Peoples R China in 2020, Cited 14. Recommanded Product: 91-00-9. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9
SIRT6 is a deacetylase of histone H3 and inhibitors of SIRT6 have been thought as potential agents for treatment of diabetes. Herein we report the discovery of a series of new SIRT6 inhibitors containing the skeleton 1-phenylpiperazine. Among them, compound 5-(4-methylpiperazin-1-yl)-2-nitroaniline (6d) is the most potent one, which showed an IC50 value of 4.93 mu M against SIRT6 in the Fluor de Lys (FDL) assay. It displayed K-D values of 9.76 mu M and 10 mu M in surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) assays, respectively. In selectivity assay, 6d showed no activity against other members of the HDAC family (SIRT1-3 and HDAC1-11) at concentrations up to 200 mu M. In a mouse model of type 2 diabetes, 6d could significantly increase the level of glucose transporter GLUT-1, thereby reducing blood glucose. Overall, this study provides a promising lead compound for subsequent drug discovery targeting SIRT6.
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