Ex-527

Description

"EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive."

• • -Sigma Description

Ex-527 structure, photo from Sigma-Aldrich

Genes Affected

• sirt1
• sirt2
• sirt3.1
• sirt3.2
• sirt6
• HDAC

Suppliers

• Sigma e7034
• Selleck S1541
• [http://www.abcam.com/EX-527-ab141506.html?gclid=CjwKEAjw-ZqrBRDt_KjhjcbzhhISJAAlRGvldL9GZDZxp1g2z0yx0KZie-axeE-blvueltbr35eIzBoChtrw_wcB Abcam ab141506
• Reaction EI-SRT-006
• Tocris 2780

References

• Ohata et al., 2014

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