Biochem/physiol Actions Potent SIRT1 inhibitor, IC50 38 nM. More potent and selective than our current SIRT inhibitors. 200-500-fold more selective for SIRT1 than for SIRT2 or SIRT3. Does not inhibit SIRT4-7, does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. Mentioned in several reviews as well as recent Oncogene paper. EX-527 was identified in a high throughput screen. It is racemic and gives similar results and potency as the active isomer, EX-243, whereas the other isomer (designated EX-242) is inactive. |