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EX 527 (CAS 49843-98-3)

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Synonym:SIRT1 Inhibitor III
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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EX 527 sc-203044 5 mg $80
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Description
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).
Technical Information
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
Safety and Reference Information
Transport:UN 2811, Class 6.1, Packing group III
WGK Germany:3
PubChem CID:5113032
MDL Number:MFCD03009471
SMILES:C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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
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