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(S)-Selisistat

CAS No. : 848193-68-0

MCE 国际站：(S)-Selisistat

产品活性：(S)-Selisistat ((S)-EX-527) 是一种有效，选择性的 SIRT1 抑制剂，IC₅₀ 值为 98 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：Sirtuin

In Vitro: (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.

In Vivo: (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.

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