Potent cell permeable and metabolically stable specific inhibitor of hSIRT1 (IC50=98nM in vivo / IC50=38nM in vitro; compared to hSIRT2: IC50=19µM and hSIRT3: IC50=48µM) with no effect on human histone deacetylases (HDACs) class I and class II, nor NAD glycohydrolase (IC50>100µg). Inhibits the deacetylation of p53 (IC50=1µM).
Product Details
| Alternative Name: | EX-527 |
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| Formula: | C13H13ClN2O |
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| MW: | 248.7 |
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| CAS: | 49843-98-3 |
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| Purity: | ≥95% (HPLC) |
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| Purity Detail: | Racemic mixture |
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| Identity: | Identity determined by 1H-NMR. |
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| Appearance: | White to light yellow powder. |
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| Solubility: | Soluble in DMSO (10mg/ml). |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least 6 months when stored at -20°C in the dark. |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392: F. De Bellis, et al.; Cancer Res.
74, 2328 (2014),
Abstract;
Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism: M. Gertz, et al.; Proc. Natl. Acad. Sci. U S A.
110, E2772 (2013),
Abstract;
Full Text
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes: J.C. Milne, et al.; Nature
450, 712 (2007),
Abstract;
Inhibition of SIRT1 Catalytic Activity Increases p53 Acetylation but Does Not Alter Cell Survival following DNA Damage: J.M. Solomon, et al.; Mol. Cell. Biol.
26, 28 (2006),
Abstract;
Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1: A.D. Napper, et al.; J. Med. Chem.
48, 8045 (2005),
Abstract;
