Antibodies
Sirtinol
- 貨號 Cat. No.
- S2804
- 規格 Size
- 10mM/1mL~25mg
- 品牌 Brand
- Selleckchem
Description
Sirtinol
Catalog No.S2804
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively. | |||||
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| Targets | SIRT1 | SIRT2 | ||||
| IC50 | 131 μM [2] | 38 μM [1] | ||||
| In vitro | Sirtinol potently inhibits recombinant yeast Sir2p activity in vitro with IC50 of 68 μM. Unlike TSA, Sirtinol has shown no effect on human HDAC1, indicating that it is a selective sirtuin inhibitor. Unlike TSA, treatment of human primary fibroblasts with Sirtinol does not cause global changes in acetylation of histones and tubulin, nor does it induce a morphological change in the HeLa tumor cell line. [1] Sirtinol treatment at 100 μM for 24 hours causes a sustained growth arrest in MCF-7 and H1299 cells for up to 9 days after Sirtinol withdrawal. Sirtinol treatment induces increased SA-β-gal activity and expression of PAI-1 in both MCF-7 and H1299 cells, more potently than Splitomicin. Sirtinol inhibits colony formation at concentrations of 33 μM and higher in MCF-7 and H1299 cells, more effectively compared with Splitomicin. Sirtinol treatment (100 μM) significantly attenuates both basal and EGF- or IGF-I-stimulated phosphorylation of ERK, JNK/SAPK and p38 MAPK in MCF-7 and H1299 cells. Sirtinol blocks the basal and EGF-stimulated activation of Ras. Consistent, basal and EGF- or IGF-I-stimulated phosphorylation of Raf-1, MEK, SEK1/MKK4 and MKK7 is attenuated in Sirtinol-treated cells. [3]Inhibition of Sirt1 by Sirtinol enhances UV- and H2O2-induced p53 acetylation to enhance cell death in cultured skin keratinocytes. [6] Blocking of Sirt1 by Sirtinol treatment results in a significant inhibition in the growth and viability of human PCa cells while having no effect on normal prostate epithelial cells. [7] | |||||
| In vivo | Administration of Sirtinol at 1 mg/kg attenuates pro-inflammatory cytokine production and protects against hepatic injury following trauma-hemorrhage in male Sprague-Dawley rats. [4] | |||||
| Features | Sirtinol does not inhibit class I and class II HDACs. | |||||
Protocol(Only for Reference)
Kinase Assay:
| Inhibition in vitro of human Sirt2 activity | 1.5 μg of recombinant human GST-Sirt2 (amino acids 18-340) are incubated at 30°C for 2 hours in 50 μL of assay buffer (50 mM Tris-HCl, pH 8.8, 4 mM MgCl2, 0.2 mM dithiothreitol with different concentrations of Sirtinol, 50 μM NAD, and tritiated acetylated HeLa histones (1000 cpm), purified by acid extraction. HDAC activity is determined by scintillation counting of the ethyl acetate-soluble [3H]acetic acid. |
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| Assays of recombinant human Sirt1 | Recombinant His-tagged human Sirt1 is purified and assayed for deacetylase activity using the HDAC fluorescent activity assay. This assay system allows detection of a fluorescent signal upon deacetylation of a histone substrate when treated with developer. Fluorescence is measured on a fluorometric reader with excitation set at 360 nm and emission detection set at 450 nm. Reactions consist of 1 μg of Sirt1, incubated with 250 μM acetylated histone substrate, 1 mM dithiothreitol, and increasing concentrations of Sirtinol. Reactions are carried out at 37 °C for 60 minutes. Assays are performed in the presence of 200 μM NAD+ and Sirtinol at 0, 20, 75, 100, 150, or 300 μM. |
Cell Assay:
| Cell lines | LNCaP, 22Rv1, DU145, and PC3 |
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| Concentrations | Dissolved in DMSO, final concentrations ~120 μM |
| Incubation Time | 24 or 48 hours |
| Method | Cells are grown to 60% confluence and then treated with 30 μM or 120 μM sirtinol for 24 or 48 hours. Cells are trypsinized and collected. The cells are pelleted by centrifugation and resuspended in PBS (120 μL). Trypan blue (0.4% in PBS; 10 μL) is added to a smaller aliquot (10 μL) of cell suspension, and the number of cells (viable unstained and nonviable blue) are counted. |
Animal Study:
| Animal Models | Male Sprague-Dawley rats subjected to trauma-hemorrhage |
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| Dosages | 1 mg/kg |
| Administration | Administered intravenously |
| Solubility | 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 6 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 394.47 |
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| Formula | C26H22N2O2 |
| CAS No. | 410536-97-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 23 mg/mL (58 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 | 6 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | (E)-2-((2-hydroxynaphthalen-1-yl)methyleneamino)-N-(1-phenylethyl)benzamide |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.39447 | 3.9447 | 7.8894 | 11.8341 |
