EX 527
Tocris Bioscience | Catalog # 2780
Key Product Details
Description
Product Description
EX 527 is a 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). In an animal model of Huntington's disease, EX 527 rescues neuronal degeneration, extends lifespan, reduces huntingtin inclusions and prevents ventricular enlargement. EX 527 enhances p53 acetylation in response to DNA damaging agents. Orally bioavailable and brain penetrant.
Product Specifications for EX 527
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.65 | 75 | |
| Ethanol | 12.44 | 50 |
Preparing Stock Solutions for EX 527
The following data is based on the product molecular weight 248.71.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 5.36 mL | 26.80 mL | 53.61 mL |
| 3.75 mM | 1.07 mL | 5.36 mL | 10.72 mL |
| 7.5 mM | 0.54 mL | 2.68 mL | 5.36 mL |
| 37.5 mM | 0.11 mL | 0.54 mL | 1.07 mL |
Calculators
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 126 publications citing the usage of this product.
- Smith A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum. Mol. Genet. 2014 PMID: 24436303
- Napper Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J.Med.Chem. 2005 PMID: 16335928
- Zhao 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. 2013 PMID: 23311358
- Solomon Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol.Cell.Biol. 2006 PMID: 16354677
Product Documents for EX 527
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for EX 527
For research use only
Citations for EX 527
Customer Reviews for EX 527 (1)
Have you used EX 527?
Submit a review and receive an Amazon gift card!
$25/€18/£15/$25CAN/¥2500 Yen for a review with an image
$10/€7/£6/$10CAN/¥1110 Yen for a review without an image
Submit a review
Customer Images
-
Species: HumanAssay Type: In VitroCell Line/Tissue: HepG2, and Huh,Verified Customer | Posted 11/30/2022Dissolved in DMSO and used in hepatocellular carcinoma cell lines at a concentration of 50-100 uM.
There are no reviews that match your criteria.