(S)-Selisistat ((S)-EX-527) is a potent and selective SIRT1 inhibitor, with an IC 50 of 98 nM. In Vitro (S)-Selisistat is an inhibitor of SIRT1 enzymatic activity (IC 50 , 98 nM), identified in a high-throughput screen using bacterially expressed human SIRT1. (S)-Selisistat inhibits SIRT1 in a concentration-dependent manner with an IC 50 of 38 nM, in agreement with the activity on bacterially expressed SIRT1. (S)-Selisistat has much lower potency against SIRT2 (IC 50 , 19.6 μM) or SIRT3 (IC 50 , 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:SIRT1 98 nM (IC 50 )
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(S)-Selisistat
CAS number:848193-68-0 molecular formula:C13H13ClN2O
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| Chinese alias | (S)-塞利司他 | ||
| English alias | HY-15452A | Selisistat, (S)- | BRD-K76964878-001-01-8 | BDBM50309833 | MS-23523 | EX-527 (S-enantiomer) | EX-527 (S) | EX-527(S) | 4bvb | Selisistat S-enantiomer(EX-527 S-enantiomer) | (S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide | EX-527 S- | ||
| CAS number | 848193-68-0 | molecular formula | C13H13ClN2O |
| molecular weight | 248.71 g/mol | Exact mass | ≥98% |
| PSA | 58.900 Ų | logp | 2.500 |
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