LKT Labs

Biochemicals for Life Science Research

EX-527

Product ID E9201
Cas No. 49843-98-3
Purity ≥99%
Product Unit SizeCostQuantityStock
5 mg $92.70 In stock
25 mg $278.10 In stock
Bulk Quote

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Description

EX-527 is an inhibitor of sirtuin 1 (SIRT1); sirtuins are considered class III histone deacetylases (HDACs). EX-527 binds the NAD+ site of sirtuin 1, stabilizing a closed conformation. EX-527 exhibits immunostimulatory and anti-inflammatory activities. In animal models of autoimmune colitis and inflammatory bowel disease, EX-527 increases the number of Foxp3+ Treg cells and prevents weight loss. In animal models of polycystic kidney disease, this compound delays renal cyst formation and growth. Additionally, EX-527 improves myocardial histology and increases the number of Foxp3+ Treg cells in animal models of transplant surgery, prolonging allograft survival.

Product Info

Cas No.

49843-98-3
Purity

≥99%
Formula

C13H13ClN2O
Formula Wt.

248.71
IUPAC Name

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

Selisistat
Solubility

DMSO 49 mg/mL (197.01 mM) Ethanol 18 mg/mL (72.37 mM) Water Insoluble
Appearance

White to off white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

E9201 MSDS PDF
Info Sheet

E9201 Info Sheet PDF

References

Akimova T, Xiao H, Liu Y, et al. Targeting sirtuin-1 alleviates experimental autoimmune colitis by induction of Foxp3+ T-regulatory cells. Mucosal Immunol. 2014 Feb 19. [Epub ahead of print]. PMID: 24549276.

Gertz M, Fischer F, Nguyen GT, et al. Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Proc Natl Acad Sci U S A. 2013 Jul 23;110(30):E2772-81. PMID: 23840057.

Zhou X, Fan LX, Sweeney WE Jr, et al. Sirtuin 1 inhibition delays cyst formation in autosomal-dominant polycystic kidney disease. J Clin Invest. 2013 Jul 1;123(7):3084-98. PMID: 23778143.

Beier UH, Wang L, Bhatti TR, et al. Sirtuin-1 targeting promotes Foxp3+ T-regulatory cell function and prolongs allograft survival. Mol Cell Biol. 2011 Mar;31(5):1022-9. PMID: 21199917.

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