Synonyms: compound 4 [Ng et al., 2013] [5] | GSK2245840 | SRT-2104
Compound class:
Synthetic organic
Comment: SRT2104 (GSK2245840) is an investigational, selective and orally available SIRT1 activator [4-5].
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Bioactivity Comments |
SRT2104 increases SIRT1 activation by 50% above control (EC1.5) at a concentration of 430nM [5]. It is selective for SIRT1 over SIRT2, SIRT3, and a panel of 39 additional targets. SRT2104 reduces p65/RelA acetylation levels [4]. It improves whole-body physiology and extends lifespan in mice fed a standard diet [4] and has shown dramatic neuroprotective and pro-survival effects in a mouse model of Huntington's disease [2]. No hERG, cytochrome P450, or mutagenic liabilities have been detected [5]. |
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