Selisistat S-enantiomer

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EX-527 S-对映体是 EX-527 的 S-对映体，对 SIRT1 的 IC50 为 123 nM。

EX-527 S-enantiomer is the S-enantiomer of EX-527, which is a potent and selective SIRT1 inhibitor and with no inhibition on SIRT3 and SIRT3.

(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.

(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.

EX-527(S) | (S)-Selisistat | EX 527(S)

Chromatin/Epigenetic

Sirtuin

SIRT1

Cancer

——

848193-68-0

248.71

C13H13ClN2O

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 402.07 mM

C1C[C@@H](C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

(S)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years