(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.
產(chǎn)品描述:
(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.
靶點:
SIRT1:98 nM (IC50);Sirtuin
體內研究:
(S)-Selisistat abolishes Resveratrol (RSV)-induced attenuation of microvascular inflammation in ob/ob septic mice. Finally, ob/ob mice in Sepsis+RSV group has significantly increased 7-day survival vs. Sepsis+Vehicle group
參考文獻:
1. Solomon JM, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006 Jan;26(1):28-38. 2. Jia Y, et al. SIRT1 is a regulator in high glucose-induced inflammatory response in RAW264.7 cells. PLoS One. 2015 Mar 20;10(3):e0120849. 3. Wang X, et al. Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice. Obesity (Silver Spring). 2015 Jun;23(6):1209-17. 4. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54.