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EX 527 (SEN0014196)SIRT1 inhibitor

EX 527 (SEN0014196)

Catalog No. A4181
Size Price Stock Qty
10mM (in 1mL DMSO) $50.00 In stock
10mg $50.00 In stock
25mg $110.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

EX 527 (SEN0014196)

Biological Activity

Description EX 527 is a potent and selective inhibitor of SIRT1 with an IC50 value of 38 nM.
Targets SIRT1          
IC50 38 nM          

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Chemical Properties

Cas No. 49843-98-3 SDF Download SDF
Synonyms EX-527,SIRT1 Inhibitor III,SEN0014196,EX527
Chemical Name 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Canonical SMILES C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N
Formula C13H13ClN2O M.Wt 248.71
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

EX 527 (SEN0014196) is a novel, potential, and specific small-molecule inhibitor of SIRT1 catalytic activity to examine the role of SIRT1 in p53 acetylation and cell survival after DNA damage. Significantly, inhibition of SIRT1 catalytic activity by EX 527 had no effect on cell growth, viability, or p53-controlled gene expression in cells treated with etoposide. EX-527 is found to be 200- to 500-fold more selective for SIRT1 than SIRT2 and SIRT3. EX-527 is a racemic mixture, and its optical isomers were separated by chiral high-performance liquid chromatography and designated EX-242 and EX-243.

Reference

Jonathan M. Solomon, Rao Pasupuleti, Lei Xu, Thomas McDonagh, Rory Curtis, Peter S. DiStefano, L. Julie Huber. Inhibition of SIRT1 Catalytic Activity Increases p53 Acetylation but Does Not Alter Cell Survival following DNA Damage. Molecular Cellular Biology January 2006 vol. 26 no. 1 28-38.