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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
|Storage||Store at +4°C|
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|
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||26.8 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|
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
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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:
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
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
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
Sun et al (2018) The role of autophagy during murine primordial follicle assembly. Aging (Albany NY) 10 197 PMID: 29410391
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
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
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
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
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
Weinberg et al (2015) Evidence for a neuroprotective microRNA pathway in amnestic mild cognitive impairment. Front Neurosci 9 430 PMID: 26594146
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
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
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
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
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Literature in this Area
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