EX 527

Name: EX 527
Brand: Tocris Bioscience
SKU: 2780
Rating: 4 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2780

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Citations (159)

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Selective SIRT1 inhibitor

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Key Product Details

Description:	Selective SIRT1 inhibitor
Chemical Name:	6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	248.71

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Technical Data
Citations / Reviews (1)

Biological Activity for EX 527

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.

Technical Data for EX 527

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for EX 527

	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 will 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

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References for EX 527

References are publications that support the biological activity of the 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