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Cat. No. Name Size Price Add Cart
KI3440EX 527QuoteQuote

Chemical Characteristic

Product NameEX 527
CAS No.49843-98-3
Molecular Weight 248.71
FormulaC13H13ClN2O
Chemical Name6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
Smiles[nH]1c2C(CCCc2c2cc(ccc12)Cl)C(=O)N
Chemical Structure

Biological activities

EX-527 is a potent and specific small-molecule inhibitor of SIRT1. EX-527 inhibits SIRT1 with an IC50 of 38 nM. EX-527 also has a lower potency against SIRT2 and SIRT3 with IC50s of 19.6 and 48.7 µM, respectively. In vitro, EX-527 increases acetylation at lysine 382 of p53 after different types of DNA damage in primary human mammary epithelial cells.[1] EX-527 also prevents resveratrol-induced up-regulation of Glut2, glucokinase, Pdx-1, and Tfam in INS-1E cells.[2] In addition, in HCT116 cells, EX-527 causes a 90% increase in cell number at a low serum concentration (about 0.1% serum), but it does not change cell number at high serum concentration (10% serum).[3] In vivo, in mice, EX-527 decreases both food intake during the dark cycle and ghrelin-induced food intake by injecting either peripherally (i.p., 10 mg/kg) or directly into the brain (i.c.v.,1.5 nmol/mouse).[4]

Protocols

In vitro, EX 527 is dissolved in DMSO.[3]

References

[1] Solomon JM, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006, 26(1):28-38.
[2] Vetterli L, et al. Resveratrol potentiates glucose-stimulated insulin secretion in INS-1E beta-cells and human islets through a SIRT1-dependent mechanism. J Biol Chem. 2011, 286(8):6049-6060.
[3] Kabra N, et al. SirT1 is an inhibitor of proliferation and tumor formation in colon cancer. J Biol Chem. 2009, 284(27):18210-18217.
[4] AuthorsDietrich MO, et al. Agrp neurons mediate Sirt1's action on the melanocortin system and energy balance: roles for Sirt1 in neuronal firing and synaptic plasticity. JournalJ Neurosci. 2010, 30(35):11815-11825.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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