Biological Activity
Selective inhibitor of SIRT1 that does not inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members (IC50 values are 98, 19600, 48700, > 100000 and > 100000 nM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Enhances p53 acetylation in response to DNA damaging agents.
Compound Libraries
EX 527 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 248.71 |
| Formula | C13H13ClN2O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 49843-98-3 |
| PubChem ID | 5113032 |
| InChI Key | FUZYTVDVLBBXDL-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(NC3=C2CCCC3C(N)=O)C2=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.65 | 75 | |
| ethanol | 12.44 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 248.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.02 mL | 20.1 mL | 40.21 mL |
| 5 mM | 0.8 mL | 4.02 mL | 8.04 mL |
| 10 mM | 0.4 mL | 2.01 mL | 4.02 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Solomon et al (2006) Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol.Cell.Biol. 26 28 PMID: 16354677
Napper et al (2005) Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J.Med.Chem. 48 8045 PMID: 16335928
Zhao et al (2013) The 2.5 Å crystal structure of the SIRT1 catalytic domain bound to nicotinamide adenine dinucleotide (NAD+) and an indole (EX527 analogue) reveals a novel mechanism of histone deacetylase inhibition. J.Med.Chem. 56 963 PMID: 23311358
Keywords: EX 527, supplier, Selective, SIRT1, inhibitors, inhibits, Sirtuin, Sir2-like, Family, Deacetylases, EX527, Selisistat, Sir2-like, Family, Deacetylases, Sir2-like, Family, Deacetylases, Tocris Bioscience
