Molecular structure of EX 527, CAS Number: 49843-98-3
EX 527 (CAS 49843-98-3)
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Alternate Names:
EX 527 is also known as SIRT1 Inhibitor III.
Application:
EX 527 is a potent inhibitor of the SIRT1 class III histone deacetylase enzyme, selective over SIRT2 and SIRT3.
CAS Number:
49843-98-3
Purity:
≥95%
Molecular Weight:
248.71
Molecular Formula:
C13H13ClN2O
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
EX 527 is a potent and selective inhibitor of the SIRT1 class III histone deacetylase enzyme, thought to block the release of deacetylated peptide and O-acetyl-ADP-ribose from the enzyme following the deacetylation process. EX 527 has been used a powerful tool for studying the relationship between SIRT1 and cell regulation. The deacetylation of cortactin, a protein responsible for rearrangements of the actin cytoskeleton, is associated with cell motility and possibly tumorigenesis, and blocking of this deacetylation by EX 527 correlated to a decrease in cell motility. Blocking of SIRT1 by EX 527 also demonstrated that deacetylation of the important tumor suppressor protein p53 is mediated by SIRT1 as well. EX 527 inhibits other sirtuin family deacetylases only at much higher concentrations (IC50 = 19.6 and 48.7 µM for SIRT2 and SIRT3, respectively).
EX 527 (CAS 49843-98-3) References
- Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. | Napper, AD., et al. 2005. J Med Chem. 48: 8045-54. PMID: 16335928
- Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. | Solomon, JM., et al. 2006. Mol Cell Biol. 26: 28-38. PMID: 16354677
- Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. | Milne, JC., et al. 2007. Nature. 450: 712-6. PMID: 18046409
- Deacetylation of cortactin by SIRT1 promotes cell migration. | Zhang, Y., et al. 2009. Oncogene. 28: 445-60. PMID: 18850005
- Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. | Gertz, M., et al. 2013. Proc Natl Acad Sci U S A. 110: E2772-81. PMID: 23840057
- Inhibition of NAMPT aggravates high fat diet-induced hepatic steatosis in mice through regulating Sirt1/AMPKα/SREBP1 signaling pathway. | Wang, LF., et al. 2017. Lipids Health Dis. 16: 82. PMID: 28449683
- The SIRT1 inhibitor EX-527 suppresses mTOR activation and alleviates acute lung injury in mice with endotoxiemia. | Huang, J., et al. 2017. Innate Immun. 23: 678-686. PMID: 28952835
- 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. | Tian, L., et al. 2019. J Pharmacol Sci. 139: 352-360. PMID: 30910451
- SIRT1/PGC-1 pathway activation triggers autophagy/mitophagy and attenuates oxidative damage in intestinal epithelial cells. | Liang, D., et al. 2020. Biochimie. 170: 10-20. PMID: 31830513
- Protective effect of EX-527 against high-fat diet-induced diabetic nephropathy in Zucker rats. | Kundu, A., et al. 2020. Toxicol Appl Pharmacol. 390: 114899. PMID: 31981641
- EX-527 Prevents the Progression of High-Fat Diet-Induced Hepatic Steatosis and Fibrosis by Upregulating SIRT4 in Zucker Rats. | Kundu, A., et al. 2020. Cells. 9: PMID: 32365537
- Baicalin Ameliorates Cognitive Impairment and Protects Microglia from LPS-Induced Neuroinflammation via the SIRT1/HMGB1 Pathway. | Li, Y., et al. 2020. Oxid Med Cell Longev. 2020: 4751349. PMID: 33029280
- Polysulfide-mediated sulfhydration of SIRT1 prevents diabetic nephropathy by suppressing phosphorylation and acetylation of p65 NF-κB and STAT3. | Sun, HJ., et al. 2021. Redox Biol. 38: 101813. PMID: 33279869
- Glycyrrhizin improves the pathogenesis of psoriasis partially through IL-17A and the SIRT1-STAT3 axis. | Qiong, H., et al. 2021. BMC Immunol. 22: 34. PMID: 34044769
- Down-regulation of Risa improves podocyte injury by enhancing autophagy in diabetic nephropathy. | Su, PP., et al. 2022. Mil Med Res. 9: 23. PMID: 35614465
Inhibitor of:
1200013P24Rik, 2310042D19Rik, Ataxin-7, CRY1, DHRS6, ERRβ, EYA1, FNDC1, G6Pase-β, H2al3, IGFL2, LEUTX, LOC100041376, LOC150383_2210021J22Rik, Med17, MYBBP1A, NAT-13, NMNAT-3, NP220, SG2NA, Sir2, Sir3, SIRT1, SIRT3, SIRT4, SIRT5, SIRT6, SIRT7, Sox-8, SUT-1, TAF II p70, TAF9A, TMEM59, TMEM98, TRF2, and Vmn2r109.Activator of:
HoxD8, Set2, Sir4, and VSTM1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
EX 527, 5 mg | sc-203044 | 5 mg | $85.00 |