(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC50 of 98 nM.
IC50&Target
SIRT1
98 nM (IC50)
体外研究
(S)-Selisistat is an inhibitor of SIRT1 enzymatic activity (IC50, 98 nM), identified in a high-throughput screen using bacterially expressed human SIRT1. (S)-Selisistat inhibits SIRT1 in a concentration-dependent manner with an IC50 of 38 nM, in agreement with the activity on bacterially expressed SIRT1. (S)-Selisistat has much lower potency against SIRT2 (IC50, 19.6 μM) or SIRT3 (IC50, 48.7 μM) but does not inhibit class I/II HDAC activity at concentrations up to 100 μM. (S)-Selisistat exerts an inhibitory effect on SIRT1 activity without affecting SIRT1 expression on both mRNA and protein levels.
体内研究
(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.
分子式
C31H41N6O3Scl
分子量
248.71
CAS号
848193-68-0
运输条件
Room temperature in continental US; may vary elsewhere.