EX 527 EX 527 is a selective inhibitor of the SIRT1 enzyme over SIRT2 and SIRT3. It is useful for studying the effects of SIRT1 on cell regulation.

EX 527  (CAS 49843-98-3)

EX 527 is rated 5.0 out of 5 by 1.
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| See 10 Citations
Synonym: SIRT1 Inhibitor III; Selisistat
Application: A selective inhibitor of SIRT1 over SIRT2 and SIRT3
CAS Number: 49843-98-3
Purity: ≥95%
Molecular Weight: 248.71
Molecular Formula: C13H13ClN2O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
EX 527 sc-203044 5 mg $80.00

EX 527 is a potent and selective inhibitor of the SIRT1 class III histone deacetylase enzyme, thought to block the release of deacetylated peptide and O-acetyl-ADP-ribose from the enzyme following the deacetylation process. EX 527 has been used a powerful tool for studying the relationship between SIRT1 and cell regulation. The deacetylation of cortactin, a protein responsible for rearrangements of the actin cytoskeleton, is associated with cell motility and possibly tumorigenesis, and blocking of this deacetylation by EX 527 correlated to a decrease in cell motility. Blocking of SIRT1 by EX 527 also demonstrated that deacetylation of the important tumor suppressor protein p53 is mediated by SIRT1 as well. EX 527 inhibits other sirtuin family deacetylases only at much higher concentrations (IC50 = 19.6 and 48.7 μM for SIRT2 and SIRT3, respectively).


References

1. Napper, Andrew D., et al., 2005. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. Journal of medicinal chemistry. 48(25): 8045-54. PMID: 16335928
2. Solomon, Jonathan M., et al., 2006. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Molecular and cellular biology. 26(1): 28-38. PMID: 16354677
3. Milne, Jill C., et al., 2007. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 450(7170): 712-6. PMID: 18046409
4. Zhang, Y., et al., 2009. Deacetylation of cortactin by SIRT1 promotes cell migration. Oncogene. 28(3): 445-60. PMID: 18850005

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), ethanol (5 mg/ml), DMF (~20 mg/ml), and DMSO:PBS (1:1 pH 7.2) (~0.5 mg/ml).
Storage :
Store at 4° C
Melting Point :
178° C
Boiling Point :
531.72° C at 760 mmHg (Predicted)
Density :
1.39 g/cm3 (Predicted)
Refractive Index :
n20D 1.69 (Predicted)
IC50 :
SIRT1: IC50 = 98 nM; SIRT2: IC50 = 19.6 µM; SIRT3: IC50 = 48.7 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
5113032
MDL Number :
MFCD03009471
SMILES :
C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

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Certificate of Analysis

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EX 527 Product Citations

See how others have used EX 527. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 10 total

PMID: # 26891914
Graham, RM. et al. 2016. Resveratrol augments ER stress and the cytotoxic effects of glycolytic inhibition in neuroblastoma by downregulating Akt in a mechanism independent of SIRT1. Experimental & molecular medicine. 48: e210.

PMID: # 26307266
Guida, N. et al. 2015. Resveratrol via sirtuin-1 downregulates RE1-silencing transcription factor (REST) expression preventing PCB-95-induced neuronal cell death. Toxicology and applied pharmacology. 288: 387-98.

PMID: # 26052531
Wielgosz, MM. et al. 2015. Generation of a lentiviral vector producer cell clone for human Wiskott-Aldrich syndrome gene therapy. Molecular therapy. Methods & clinical development. 2: 14063.

PMID: # 25401748
Yang, Y. et al. 2015. Melatonin prevents cell death and mitochondrial dysfunction via a SIRT1-dependent mechanism during ischemic-stroke in mice. Journal of pineal research. 58: 61-70.

PMID: # 25710021
He, W. et al. 2015. Advanced glycation end products induce endothelial-to-mesenchymal transition via downregulating Sirt 1 and upregulating TGF-β in human endothelial cells. BioMed research international. 2015: 684242.

PMID: # 24990896
Quadri, S. et al. 2014. Regulation of (pro)renin receptor expression in mIMCD via the GSK-3β-NFAT5-SIRT-1 signaling pathway. American journal of physiology. Renal physiology. 307: F593-600.

PMID: # 24982422
Rodríguez, M. et al. 2014. The Unfolded Protein Response and the Phosphorylations of Activating Transcription Factor 2 in the trans-Activation of il23a Promoter Produced by β-Glucans J Biol Chem.. 289: 22942-22957.

PMID: # 22893703
Alvarez, Y. et al. 2012. Sirtuin 1 is a key regulator of the interleukin-12 p70/interleukin-23 balance in human dendritic cells. The Journal of biological chemistry. 287: 35689-701.

PMID: # 21320266
Kim, D. et al. 2011. Therapeutic potential of panduratin A, LKB1-dependent AMP-activated protein kinase stimulator, with activation of PPARα/δ for the treatment of obesity. Diabetes Obes Metab. 13: 584-593.

PMID: # 21320266
Kim, D. et al. 2011. Therapeutic potential of panduratin A, LKB1-dependent AMP-activated protein kinase stimulator, with activation of PPARα/δ for the treatment of obesity. Diabetes, obesity & metabolism. 13: 584-93.

Citations 1 to 10 of 10 total
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Rated 5 out of 5 by from Atkins Atkins, KM. et al. (PubMed 25159152) found that EX 527, a selective inhibitor of SIRT1 deacetylation activity, restored p53 acetylation and p21 induction, as well as p21-dependent cell cycle arrest in PACS-2 knockdown cells. -SCBT Publication Review
Date published: 2015-01-02
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