Selisistat ( EX-527 )
Selisistat was the first identified potent and cell permeable SIRT1-specific inhibitor with IC50 of 98 nM.
For research use only. We do not sell to patients.
Chemical Information
| Name | Selisistat ( EX-527 ) |
|---|---|
| Iupac Chemical Name | 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
| Synonyms | EX-527; EX527; EX 527; Selisistat |
| Molecular Formula | C13H13ClN2O |
| Molecular Weight | 248.71 |
| Smile | O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N |
| InChiKey | FUZYTVDVLBBXDL-UHFFFAOYSA-N |
| 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) |
| CAS Number | 49843-98-3 |
| Related CAS | 49843-98-3 (racemate) ; 848193-69-1 (R-isomer) ; 848193-68-0 (S-isomer) ; |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | off-white solid |
|---|---|
| Purity | ≧98.0% |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | DMSO 300 mg/mL (1206.22 mM) ; Water Insoluble ; Ethanol 30 mg/mL (120.62 mM) |
| Handling | Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. |
| Shipping Condition | Shipped under ambient temperature |
| HS Code | 2934200090 |
| Targets | SirT1 inhibitor |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
[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 Jan;26(1):28-38.
[2]. Jia Y, et al. SIRT1 is a regulator in high glucose-induced inflammatory response in RAW264.7 cells. PLoS One. 2015 Mar 20;10(3):e0120849.
[3]. Wang X, et al. Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice. Obesity (Silver Spring). 2015 Jun;23(6):1209-17.
[4]. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54.
[5]. Huang J, Tian R, Yang Y, Jiang R, Dai J, Tang L, Zhang L. The SIRT1 inhibitor EX-527 suppresses mTOR activation and alleviates acute lung injury in mice with endotoxiemia. Innate Immun. 2017 Nov;23(8):678-686. doi: 10.1177/1753425917733531. Epub 2017 Sep 27.
[6].Tao YF, Lin F, Yan XY, Gao XG, Teng F, Fu ZR, Wang ZX. Galectin-9 in Combination With EX-527 Prolongs the Survival of Cardiac Allografts in Mice After Cardiac Transplantation. Transplant Proc. 2015 Jul-Aug;47(6):2003-9. doi: 10.1016/j.transproceed.2015.04.091.
[7].Ohata Y, Matsukawa S, Moriyama Y, Michiue T, Morimoto K, Sato Y, Kuroda H. Sirtuin inhibitor Ex-527 causes neural tube defects, ventral edema formations, and gastrointestinal malformations in Xenopus laevis embryos. Dev Growth Differ. 2014 Aug;56(6):460-8. doi: 10.1111/dgd.12145. Epub 2014 Aug 5.
[8]. Gertz M, Fischer F, Nguyen GT, Lakshminarasimhan M, Schutkowski M, Weyand M, Steegborn C. Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Proc Natl Acad Sci U S A. 2013 Jul 23;110(30):E2772-81. doi: 10.1073/pnas.1303628110. Epub 2013 Jul 9.
Chemical Structure
