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EX-527

SIGMA/E7034 - ≥98% (HPLC)

Synonym: 6-Chloro-2,3,4,9-tetrahydro-1H-Carbazole-1-carboxamide

CAS Number: 49843-98-3
Empirical Formula (Hill Notation): C13H13ClN2O
Molecular Weight: 248.71
MDL Number: MFCD03009471
Linear Formula: C13H13ClN2O
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-E7034-5MG 5 mg
 $123.00
1/EA		 Add To Favorites
45-E7034-25MG 25 mg
 $503.00
1/EA		 Add To Favorites

 

assay ≥98% (HPLC)
color white to beige
form powder
InChI 1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)
InChI key FUZYTVDVLBBXDL-UHFFFAOYSA-N
Quality Level 100 
SMILES string NC(=O)C1CCCc2c1[nH]c3ccc(Cl)cc23
solubility DMSO: >20 mg/mL
storage temp. 2-8°C
Application: EX-527 has been used:
• in 1% dimethyl sulfoxide, 30%, polyethylene glycol-400 and 1% Tween 80 for treating C57BL/6 N mice to study its effect on intestinal morphological changes and crypt cell apoptosis
• as a an inhibitor of sirtuin 1, in treating human cancer lines MCF-7 (Michigan cancer foundation-7) and HCT116 (colon cancer cell line) incubated in Dulbecco′s modified Eagle′s medium, to study its effect on mitochondrial ATP (adenosine triphosphate) production
• Intracerebroventricularly infused in rat model of epileptogenesis, to access kainic acid–induced status epilepticus stimulated sirtuin 1 activity
Biochem/physiol Actions: EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.
Biochem/physiol Actions: Potent SIRT1 and SIRT6 inhibitor.
Features and Benefits: This compound is a featured product for Gene Regulation research. Click here  to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm .
Packaging: 5, 25 mg in glass bottle
Hazard Codes Xn
Risk Statements 22-36
Safety Statements 26
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352200

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