tcsc0960 Selisistat

Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC₅₀ of 98 nM.

IC50 & Target: IC50: 98 nM (SIRT1), 19.6 μM (SIRT2), 48.7 μM (SIRT3)^[4]

In Vitro: Selisistat (EX-527) is an inhibitor of SIRT1 enzymatic activity (IC₅₀, 98 nM), identified in a high-throughput screen using bacterially expressed human SIRT1. Selisistat (EX-527) inhibits SIRT1 in a concentration-dependent manner with an IC₅₀ of 38 nM, in agreement with the activity on bacterially expressed SIRT1. Selisistat (EX-527) 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^[1]. Selisistat (EX-527) exerts an inhibitory effect on SIRT1 activity without affecting SIRT1 expression on both mRNA and protein levels^[2].

In Vivo: Selisistat (EX-527) 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^[3].