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

SIRT inhibitor
 
ALX-270-437-M001 1 mg 132.00 USD
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Potent cell permeable and metabolically stable specific inhibitor of hSIRT1 (IC50=98nM in vivo / IC50=38nM in vitro; compared to hSIRT2: IC50=19µM and hSIRT3: IC50=48µM) with no effect on human histone deacetylases (HDACs) class I and class II, nor NAD glycohydrolase (IC50>100µg). Inhibits the deacetylation of p53 (IC50=1µM).

Product Specification

Alternative Name:EX-527
 
Formula:C13H13ClN2O
 
MW:248.7
 
CAS:49843-98-3
 
Purity:≥95%
 
Purity Detail:Racemic mixture
 
Identity:Identity determined by MS, 1H- and 13C-NMR.
 
Appearance:White to beige powder.
 
Solubility:Soluble in DMSO (10mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 6 months when stored at -20°C in the dark.
 
Handling:Protect from light.
 
270-437
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270-437

Product Literature References

Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392: F. De Bellis, et al.; Cancer Res. 74, 2328 (2014), Abstract;
Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism: M. Gertz, et al.; Proc. Natl. Acad. Sci. U S A. 110, E2772 (2013), Abstract; Full Text
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes: J.C. Milne, et al.; Nature 450, 712 (2007), Abstract;
Inhibition of SIRT1 Catalytic Activity Increases p53 Acetylation but Does Not Alter Cell Survival following DNA Damage: J.M. Solomon, et al.; Mol. Cell. Biol. 26, 28 (2006), Abstract;
Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1: A.D. Napper, et al.; J. Med. Chem. 48, 8045 (2005), Abstract;

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