General Description
A cell-permeable quinolinecarboxamide compound that is shown to inhibit the mitochondrial SIRT3 in a substrate AceCS2-competitive (
Ki = 0.56 μM;
Km = 2.44 μM), but NAD
+-uncompetitive (
Ki = 0.34 μM;
Km = 280 μM), manner. Also reported to decrease cellular p53 Lys382 acetylation (Effective conc. = 10 μM in U2OS and MEF cultures) and inhibit p300 HAT activity (IC
50 = 9 μM)
in vitro, as well as offer therapeutic benefits in several murine and rodent type 2 diabetes models (100 mg/kg/dayl p.o.)
in vivo. Whether and how SRT1720 activates SIRT1 activity remains uncertain. Also available as a 25 mM solution in DMSO (Cat. No.
530748).
![N-[2-[3-(1-Piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-quinoxalinecarboxamide Structure](https://www.chemicalbook.com/CAS/GIF/925434-55-5.gif)
