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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.
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