Home / Class III Histone Deacetylases Inhibitors / EX 527

EX 527

Catalog #: 2780
26 Citations Datasheet
Catalog # Availability Size / Price Qty
2780/10
2780/50
2780/1
EX 527 | CAS No. 49843-98-3 | Class III Histone Deacetylases Inhibitors
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Description: Selective SIRT1 inhibitor

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

Purity: ≥98%

Product Details
Citations (26)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
248.71
Formula:
C13H13ClN2O
Solubility:
Soluble to 75 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
49843-98-3

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.

Product Datasheets

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Citations for EX 527

The citations listed below are publications that use Tocris products. Selected citations for EX 527 include:

26 Citations: Showing 1 - 10

  1. The role of autophagy during murine primordial follicle assembly.
    Authors: Sun Et al.
    Aging (Albany NY)  2018;10:197
  2. The metal nanoparticle-induced inflammatory response is regulated by SIRT1 through NF-κB deacetylation in aseptic loosening.
    Authors: Deng Et al.
    Int J Nanomedicine  2017;12:3617
  3. Microglial CX3CR1 promotes adult neurogenesis by inhibiting Sirt 1/p65 signaling independent of CX3CL1.
    Authors: Sellner Et al.
    Acta Neuropathol Commun  2016;4:102
  4. Evidence for a neuroprotective microRNA pathway in amnestic mild cognitive impairment.
    Authors: Weinberg Et al.
    Front Neurosci  2015;9:430
  5. SIRT1 deacetylates and stabilizes hypoxia-inducible factor-1α (HIF-1α) via direct interactions during hypoxia.
    Authors: Joo Et al.
    J Exp Med  2015;462:294
  6. Essential role of mitochondrial energy metabolism in Foxp3+ T-regulatory cell function and allograft survival.
    Authors: Beier Et al.
    FASEB J  2015;29:2315
  7. SIRT1 deacetylates RORγt and enhances Th17 cell generation.
    Authors: Lim Et al.
    Mol Cell Biol  2015;212:607
  8. Mir-34a mimics are potential therapeutic agents for p53-mutated and chemo-resistant brain tumour cells.
    Authors: Fan Et al.
    PLoS One  2014;9:e108514
  9. Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1.
    Authors: Jiang and Zsombok
    Front Neurosci  2014;7:270
  10. Targeting sirtuin-1 alleviates experimental autoimmune colitis by induction of Foxp3+ T-regulatory cells.
    Authors: Akimova Et al.
    Mucosal Immunol  2014;7:1209
  11. IF. regulatory factor 9 is critical for neointima formation following vascular injury.
    Authors: Zhang Et al.
    Nat Commun  2014;5:5160
  12. A critical role for IF. regulatory factor 9 in cerebral ischemic stroke.
    Authors: Chen Et al.
    J Neurosci  2014;34:11897
  13. Novel role of silent information regulator 1 in acute endothelial cell oxidative stress injury.
    Authors: Li Et al.
    Biochim Biophys Acta  2014;1842:2246
  14. Defective expression of SIRT1 contributes to sustain inflammatory pathways in the gut.
    Authors: Caruso Et al.
    Mucosal Immunol  2014;
  15. Impaired cardiac SIRT1 activity by carbonyl stress contributes to aging-related ischemic intolerance.
    Authors: Gu Et al.
    PLoS One  2013;8:e74050
  16. SirT1 mediates hyperbaric oxygen preconditioning-induced ischemic tolerance in rat brain.
    Authors: Yan Et al.
    J Cereb Blood Flow Metab  2013;33:396
  17. A high-confidence interaction map identifies SIRT1 as a mediator of acetylation of USP22 and the SAGA coactivator complex.
    Authors: Armour Et al.
    Proc Natl Acad Sci U S A  2013;33:1487
  18. Pro-autophagic polyphenols reduce the acetylation of cytoplasmic proteins.
    Authors: Pietrocola Et al.
    Cell Cycle  2012;11:3851
  19. Coronavirus nsp6 proteins generate autophagosomes from the endoplasmic reticulum via an omegasome intermediate.
    Authors: Cottam Et al.
    Autophagy  2011;7:1335
  20. Resveratrol reverses monocrotaline-induced pulmonary vascular and cardiac dysfunction: a potential role for atrogin-1 in smooth muscle.
    Authors: Paffett Et al.
    Vascul Pharmacol  2011;56:64
  21. SIRT1 deacetylates the DNA methyltransferase 1 (DNMT1) protein and alters its activities.
    Authors: Peng Et al.
    Mol Cell Biol  2011;31:4720
  22. NAD+-dependent SIRT1 deacetylase participates in epigenetic reprogramming during endotoxin tolerance.
    Authors: Liu Et al.
    J Biol Chem  2011;286:9856
  23. Purkinje cell-specific males absent on the first (mMof) gene deletion results in an ataxia-telangiectasia-like neurological phenotype and backward walking in mice.
    Authors: Kumar Et al.
    Front Mol Neurosci  2011;108:3636
  24. Agrp neurons mediate Sirt1's action on the melanocortin system and energy balance: roles for Sirt1 in neuronal firing and synaptic plasticity.
    Authors: Dietrich Et al.
    J Neurosci  2010;30:11815
  25. Transcriptional corepressor SMILE recruits SIRT1 to inhibit nuclear receptor estrogen receptor-related receptor gamma transactivation.
    Authors: Xie Et al.
    J Biol Chem  2009;284:28762
  26. STAT3 inhibition of gluconeogenesis is downregulated by SirT1.
    Authors: Nie Et al.
    Nat Cell Biol  2009;11:492

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