I agree Our site saves small pieces of text information (cookies) on your device in order to deliver better content and for statistical purposes. You can disable the usage of cookies by changing the settings of your browser. By browsing our website without changing the browser settings you grant us permission to store that information on your device.
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.
Marcus Freitag.; Jorg Schemies.; Tim Larsen.; Khattab El Gaghlab.; Felix Schulz.; Tobias Rumpf.; Manfred Jung.; Andreas Link. Synthesis and biological activity of splitomicin analogs targeted at human NAD+-dependent histone deacetylases (sirtuins). Cell Calcium. 2011 19, (12), 3669-3677.
Mohosin Layek.; Y. Syam Kumar.; Aminul Islam.; Ravikumar Karavarapu.; Amrita Sengupta.; Devyani Halder.; K. Mukkanti.; Manojit Pal. Alkynylation of N-(3-iodopyridin-2-yl)sulfonamide under Pd/C-Cu catalysis: a direct one pot synthesis of 7-azaindoles and their pharmacological evaluation as potential inhibitors of sirtuins. 2011, 2, 478-485.
Gefahrenhinweise (EU): H302-H319
Harmful if swallowed. Causes serious eye irritation.
Wear eye/face protection. Wash thoroughly after handling. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF SWALLOWED: Call a POISON CENTER/doctor if you feel unwell. If eye irritation persists: Get medical advice/attention. Dispose of contents/container in accordance with local/regional/national/international regulations.