(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
EX-527(Selisistat)
CAS: 49843-98-3
Molecular Formula: C13H13ClN2O
(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - Names and Identifiers
(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - Physico-chemical Properties
| Molecular Formula | C13H13ClN2O |
| Molar Mass | 248.71 |
| Density | 1.388 |
| Melting Point | 179.0 to 183.0 °C |
| Boling Point | 531.7±38.0 °C(Predicted) |
| Solubility | Soluble in DMSO (10 mg/ml), ethanol (5 mg/ml), DMF (~20 mg/ml), and DMSO:PBS (1:1 pH |
| Appearance | powder |
| Color | white to beige |
| pKa | 16.12±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months |
| MDL | MFCD03009471 |
| Use | A selective inhibitor of SIRT1 over SIRT2 and SIRT3 |
| In vitro study | EX 527 effectively inhibit SIRT1 deacetylase activity, IC50 is 38 nM, this effect is concentration-dependent, and inhibit SIRT2 and SIRT3, the effect is much lower, the IC50 was 19.6 μm and 48.7 μm, respectively. EX 527 concentrations up to 100 μm also did not inhibit SIRT4-7 and Class I/II HDAC activity. 1 μm EX-527 alone, acting on NCI-H460 cells, could not detect the acetylation of p53 at the lysine 382 site. EX-527 acts on NCI-H460 cells, human mammary epithelial cells, U-2 OS and MCF-7 cells affected by the genotoxic reagents Etoposide, Adriamycin, Hydroxyurea, and H2O2, and significantly increases the amount of acetylated p53. However, the EX 527 had no detectable effect on p53-controlled gene expression, cell survival, or cell proliferation. EX 527 treated in 0.1 serum instead of 10% serum for 7 days, acting on HCT116 cells, significantly increasing the cell number by up to 90%, indicating that in the absence of cytokines, sirT1 is a significant regulator of cell proliferation. EX 527 acts on INS-1E cells, abrogating the effects of resveratrol in response to glucose, and inhibiting resveratrol-induced up-regulation of Glut2, glucokinase, Pdx-1, and Tfam, because the effects of EX 527 and resveratrol on SIRT1 deacetylase activity are opposite. |
| In vivo study | EX 527 at a dose of 10 μg in rats increases hypothalamic acetylation-p53 levels by inhibiting hypothalamic SIRT1 activity. The combined treatment of EX 527 and Ghrelin decreased pAMPK level, increased ACC level, and abolished the transcription factors FoxO1, pCREB, and Bsx, as well as the higher expression of neuropeptides NPY and AgRP in the arcuate nucleus of hypothalamus, and significantly attenuate the appetite-promoting effect of ghrelin. |
(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - Reference
| Reference Show more | 1. Wang, Si-wei, et al. "Hesperetin, a SIRT1 activator, inhibits hepatic inflammation via AMPK/CREB pathway." International Immunopharmacology 89 (2020): 107036.https://doi.org/10.1016/j.intimp.2020.107036 2. [IF=3.943] Si-wei Wang et al."Hesperetin, a SIRT1 activator, inhibits hepatic inflammation via AMPK/CREB pathway."Int Immunopharmacol. 2020 Dec;89:107036 |
(S)-6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - Introduction
EX 527 (Selisistat) is an effective and selective SIRT1 inhibitor with an IC50 of 38 nM, which is more than 200 times more selective than SIRT2 and SIRT3.
Last Update：2022-10-16 17:41:41
Supplier List
Spot supply
Product Name: EX-527(Selisistat) Visit Supplier Webpage Request for quotationCAS: 49843-98-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: EX-527(Selisistat) Visit Supplier Webpage Request for quotationCAS: 49843-98-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History