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EX 527 (SEN0014196)

EX 527 (SEN0014196)

Catalog Number:
L002369076APE
Mfr. No.:
APE-A4181
Price:
$180
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      • Overview

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          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.

      • Properties
        • Alternative Name
          EX-527, SIRT1 Inhibitor III, SEN0014196, EX527; 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
          CAS Number
          49843-98-3
          Molecular Formula
          C13H13ClN2O
          Molecular Weight
          248.71
          Appearance
          A solid
          Purity
          99.72%
          Solubility
          insoluble in H2O; ≥12.43 mg/mL in DMSO; ≥25.45 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Ying Jiang, Da Li, et al. "Perampanel Stimulates Mitochondrial Biogenesis in Neuronal Cells through Activation of the SIRT1/PGC-1α Signaling Pathway." ACS Chem Neurosci. 2021 Jan 20;12(2):323-329. PMID:33415987
          2. Yangyang Li, Lei Wang, et al. "SIRT1 Mediates Neuropathic Pain Induced by Sciatic Nerve Chronic Constrictive Injury in the VTA-NAc Pathway." Pain Res Manag 2020 Aug 18;2020:4245968. PMID:32922581
          3. Lin Y, Liu J, et al. "FADD Phosphorylation Modulates Blood Glucose Levels by Decreasing the Expression of Insulin-Degrading Enzyme." Mol Cells. 2020;43(4):373-383. PMID:32191993
          4. Xu J, Liu LQ, et al. "Metformin alleviates renal injury in diabetic rats by inducing Sirt1/FoxO1 autophagic signal axis." Clin Exp Pharmacol Physiol. 2019 Dec 10. PMID:31821581
          5. Tang Y, Yu W. "SIRT1 and p300/CBP regulate the reversible acetylation of serine-threonine kinase NDR2." Biochem Biophys Res Commun. 2019 Aug 16. pii: S0006-291X(19)31586-4. PMID:31427083
          6. Tian L, Cao W, et al. "Pretreatment with Tilianin improves mitochondrial energy metabolism and oxidative stress in rats with myocardial ischemia/reperfusion injury via AMPK/SIRT1/PGC-1 alpha signaling pathway." J Pharmacol Sci. 2019 Apr;139(4):352-360. PMID:30910451

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