EX 527

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Description: Selective SIRT1 inhibitor
Chemical Name: 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Purity: ≥98% (HPLC)
Citations (26)
Reviews (1)
Literature (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
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 Data for EX 527

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 5.36 mL 26.8 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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Product Datasheets for EX 527

Certificate of Analysis / Product Datasheet
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References for EX 527

References are publications that support the biological activity of the product.

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

Smith et al (2014) A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease. Hum. Mol. Genet. 23 2995 PMID: 24436303

If you know of a relevant reference for EX 527, please let us know.

View Related Products by Product Action

View all Class III HDAC (Sirtuin) Inhibitors

Keywords: EX 527, EX 527 supplier, Selective, SIRT1, inhibitors, inhibits, Sirtuin, Sir2-like, Family, Deacetylases, EX527, Selisistat, huntingtons, huntingtin, neurodegeneration, Class, III, HDACs, (Sirtuins), 2780, Tocris Bioscience

26 Citations for EX 527

Citations are publications that use Tocris products. Selected citations for EX 527 include:

Akimova et al (2014) Targeting sirtuin-1 alleviates experimental autoimmune colitis by induction of Foxp3+ T-regulatory cells. Mucosal Immunol 7 1209 PMID: 24549276

Li et al (2014) Novel role of silent information regulator 1 in acute endothelial cell oxidative stress injury. Biochim Biophys Acta 1842 2246 PMID: 25128742

Joo et al (2015) SIRT1 deacetylates and stabilizes hypoxia-inducible factor-1α (HIF-1α) via direct interactions during hypoxia. J Exp Med 462 294 PMID: 25979359

Lim et al (2015) SIRT1 deacetylates RORγt and enhances Th17 cell generation. Mol Cell Biol 212 607 PMID: 25918343

Chen et al (2014) A critical role for IF. regulatory factor 9 in cerebral ischemic stroke. J Neurosci 34 11897 PMID: 25186738

Fan et al (2014) Mir-34a mimics are potential therapeutic agents for p53-mutated and chemo-resistant brain tumour cells. PLoS One 9 e108514 PMID: 25250818

Caruso et al (2014) Defective expression of SIRT1 contributes to sustain inflammatory pathways in the gut. Mucosal Immunol PMID: 24850427

Zhang et al (2014) IF. regulatory factor 9 is critical for neointima formation following vascular injury. Nat Commun 5 5160 PMID: 25319116

Jiang and Zsombok (2014) Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1. Front Neurosci 7 270 PMID: 24454277

Sun et al (2018) The role of autophagy during murine primordial follicle assembly. Aging (Albany NY) 10 197 PMID: 29410391

Kumar et al (2011) Purkinje cell-specific males absent on the first (mMof) gene deletion results in an ataxia-telangiectasia-like neurological phenotype and backward walking in mice. Front Mol Neurosci 108 3636 PMID: 21321203

Weinberg et al (2015) Evidence for a neuroprotective microRNA pathway in amnestic mild cognitive impairment. Front Neurosci 9 430 PMID: 26594146

Armour et al (2013) A high-confidence interaction map identifies SIRT1 as a mediator of acetylation of USP22 and the SAGA coactivator complex. Proc Natl Acad Sci U S A 33 1487 PMID: 23382074

Liu et al (2011) NAD+-dependent SIRT1 deacetylase participates in epigenetic reprogramming during endotoxin tolerance. J Biol Chem 286 9856 PMID: 21245135

Peng et al (2011) SIRT1 deacetylates the DNA methyltransferase 1 (DNMT1) protein and alters its activities. Mol Cell Biol 31 4720 PMID: 21947282

Paffett et al (2011) Resveratrol reverses monocrotaline-induced pulmonary vascular and cardiac dysfunction: a potential role for atrogin-1 in smooth muscle. Vascul Pharmacol 56 64 PMID: 22146233

Cottam et al (2011) Coronavirus nsp6 proteins generate autophagosomes from the endoplasmic reticulum via an omegasome intermediate. Autophagy 7 1335 PMID: 21799305

Beier et al (2015) Essential role of mitochondrial energy metabolism in Foxp3+ T-regulatory cell function and allograft survival. FASEB J 29 2315 PMID: 25681462

Gu et al (2013) Impaired cardiac SIRT1 activity by carbonyl stress contributes to aging-related ischemic intolerance. PLoS One 8 e74050 PMID: 24040162

Yan et al (2013) SirT1 mediates hyperbaric oxygen preconditioning-induced ischemic tolerance in rat brain. J Cereb Blood Flow Metab 33 396 PMID: 23299244

Xie et al (2009) Transcriptional corepressor SMILE recruits SIRT1 to inhibit nuclear receptor estrogen receptor-related receptor gamma transactivation. J Biol Chem 284 28762 PMID: 19690166

Nie et al (2009) STAT3 inhibition of gluconeogenesis is downregulated by SirT1. Nat Cell Biol 11 492 PMID: 19295512

Deng et al (2017) The metal nanoparticle-induced inflammatory response is regulated by SIRT1 through NF-κB deacetylation in aseptic loosening. Int J Nanomedicine 12 3617 PMID: 28553103

Pietrocola et al (2012) Pro-autophagic polyphenols reduce the acetylation of cytoplasmic proteins. Cell Cycle 11 3851 PMID: 23070521

Dietrich et al (2010) Agrp neurons mediate Sirt1's action on the melanocortin system and energy balance: roles for Sirt1 in neuronal firing and synaptic plasticity. J Neurosci 30 11815 PMID: 20810901

Sellner et al (2016) Microglial CX3CR1 promotes adult neurogenesis by inhibiting Sirt 1/p65 signaling independent of CX3CL1. Acta Neuropathol Commun 4 102 PMID: 27639555

Do you know of a great paper that uses EX 527 from Tocris? Please let us know.

Reviews for EX 527

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Works well in hepatocellular carcinoma cell lines.
By Anonymous on 11/30/2022
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HepG2, and Huh,

Dissolved in DMSO and used in hepatocellular carcinoma cell lines at a concentration of 50-100 uM.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Rheumatoid Arthritis Poster

Rheumatoid Arthritis Poster

Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.