For research use only. Not for therapeutic Use.
Selisistat（Cat No.:I003752）, also known as EX 527 or SEN0014196, is a potent and selective inhibitor of the enzyme SIRT1. It exhibits an IC50 value of 38 nM in a cell-free assay, indicating its strong inhibitory activity against SIRT1. Notably, selisistat displays over 200-fold selectivity for SIRT1 compared to SIRT2 and SIRT3, two other members of the sirtuin family. By specifically targeting SIRT1, selisistat has the potential to modulate cellular processes and pathways regulated by SIRT1 activity, making it a valuable tool for research and potential therapeutic applications.
| Catalog Number | I003752 |
| CAS Number | 49843-98-3 |
| Synonyms | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
| Molecular Formula | C₁₃H₁₃ClN₂O |
| Purity | ≥95% |
| Target | Epigenetics |
| Solubility | DMSO: ≥ 32 mg/mL |
| Storage | 2-8°C |
| IC50 | 38 nM |
| IUPAC Name | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
| InChI | 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) |
| InChIKey | FUZYTVDVLBBXDL-UHFFFAOYSA-N |
| SMILES | C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N |
| Reference | </br>1:Galectin-9 in Combination With EX-527 Prolongs the Survival of Cardiac Allografts in Mice After Cardiac Transplantation. Tao YF, Lin F, Yan XY, Gao XG, Teng F, Fu ZR, Wang ZX.Transplant Proc. 2015 Jul-Aug;47(6):2003-9. doi: 10.1016/j.transproceed.2015.04.091. PMID: 26293089 </br>2:Sirtuin inhibitor Ex-527 causes neural tube defects, ventral edema formations, and gastrointestinal malformations in Xenopus laevis embryos. Ohata Y, Matsukawa S, Moriyama Y, Michiue T, Morimoto K, Sato Y, Kuroda H.Dev Growth Differ. 2014 Aug;56(6):460-8. doi: 10.1111/dgd.12145. Epub 2014 Aug 5. PMID: 25131500 </br>3:Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Gertz M, Fischer F, Nguyen GT, Lakshminarasimhan M, Schutkowski M, Weyand M, Steegborn C.Proc Natl Acad Sci U S A. 2013 Jul 23;110(30):E2772-81. doi: 10.1073/pnas.1303628110. Epub 2013 Jul 9. PMID: 23840057 Free PMC Article |
