EX 527A selective inhibitor of SIRT1 over SIRT2 and SIRT3

EX 527 (CAS 49843-98-3)

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Sinónimo: SIRT1 Inhibitor III; Selisistat
Solicitud: A selective inhibitor of SIRT1 over SIRT2 and SIRT3
Número de CAS: 49843-98-3
Pureza: ≥95%
Peso Molecular: 248.71
Fórmula Molecular: C13H13ClN2O
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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

Estado de Materia :
Solid
Solubilidad :
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).
ALMACENAMIENTO :
Store at 4° C
Punto de Fusión :
178° C
Punto de ebullición :
531.72° C at 760 mmHg (Predicted)
Densidad :
1.39 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.69 (Predicted)
IC50 :
SIRT1: IC50 = 98 nM; SIRT2: IC50 = 19.6 µM; SIRT3: IC50 = 48.7 µM
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
5113032
Número MDL :
MFCD03009471
SMILES :
C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

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EX 527  Menciones del Producto

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Citaciones 1 a 10 de un total de 12

PMID: # 30917412  Igarashi, M.|Miura, M.|Williams, E.|Jaksch, F.|Kadowaki, T.|Yamauchi, T.|Guarente, L.| et al. 2019. Aging Cell. 18: e12935.

PMID: # 30213795  Funato, K.|Hayashi, T.|Echizen, K.|Negishi, L.|Shimizu, N.|Koyama-Nasu, R.|Nasu-Nishimura, Y.|Morishita, Y.|Tabar, V.|Todo, T.|Ino, Y.|Mukasa, A.|Saito, N.|Akiyama, T.| et al. 2018. EMBO Rep. 19:

PMID: # 28978059  Bhanot, H. et al. 2017. Oncotarget. 8: 67639-67650.

PMID: # 26891914  Graham, RM. et al. 2016. Experimental & molecular medicine. 48: e210.

PMID: # 26307266  Guida, N. et al. 2015. Toxicology and applied pharmacology. 288: 387-98.

PMID: # 26052531  Wielgosz, MM. et al. 2015. Molecular therapy. Methods & clinical development. 2: 14063.

PMID: # 25401748  Yang, Y. et al. 2015. Journal of pineal research. 58: 61-70.

PMID: # 25710021  He, W. et al. 2015. BioMed research international. 2015: 684242.

PMID: # 24990896  Quadri, S. et al. 2014. American journal of physiology. Renal physiology. 307: F593-600.

PMID: # 24982422  Rodriguez, M. et al. 2014. J Biol Chem. 289: 22942-22957.

Citaciones 1 a 10 de un total de 12
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