EX 527

Cat. No. 2780

EX 527 C13H13ClN2O [49843-98-3]

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Chemical Name: 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

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.

Technical Data

Soluble to 75 mM in DMSO and to 50 mM in ethanol
>98 %
Store at +4°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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

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

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.

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

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

Chen et al (2014) A critical role for interferon 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.

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

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

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.

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.

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

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

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.

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

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.

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

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

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.

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Keywords: EX 527, supplier, Selective, SIRT1, inhibitors, inhibits, Sirtuin, Sir2-like, Family, Deacetylases, EX527, Selisistat, Tocris Bioscience, Sir 2-like Family Deacetylase Inhibitor products

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