Sirtinol

Catalog No.S2804 Batch:S280401

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Technical Data

Formula

C26H22N2O2
Molecular Weight 394.47 CAS No. 410536-97-9
Solubility (25°C)* In vitro DMSO 23 mg/mL (58.3 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 30%PEG300 5%Tween80 63%ddH2O
0.4mg/ml Taking the 1 mL working solution as an example, add 20 μL of 20 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 630 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
Targets
SIRT2 [1]
(Cell-free assay)		 SIRT1 [2]
(Cell-free assay)
38 μM 131 μM
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 (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[7]
  • Cell lines

    LNCaP, 22Rv1, DU145, and PC3

  • 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:

[4]
  • Animal Models

    Male Sprague-Dawley rats subjected to trauma-hemorrhage

  • Dosages

    1 mg/kg

  • Administration

    Administered intravenously

Customer Product Validation

Data from [Data independently produced by Biomed Res Int, 2014, 783459]

Data from [Data independently produced by Biochem Biophys Res Commun, 2014, 452(3), 649-54]

Data from [Data independently produced by , , Oxid Med Cell Longev, 2017, 2017:1035702]

Data from [Data independently produced by , , Sci Rep, 2016, 6:21857]

Selleck's Sirtinol has been cited by 46 publications

α-Mangostin Inhibited M1 Polarization of Macrophages/Monocytes in Antigen-Induced Arthritis Mice by Up-Regulating Silent Information Regulator 1 and Peroxisome Proliferators-Activated Receptor γ Simultaneously [ Drug Des Devel Ther, 2023, 17:563-577] PubMed: 36860800
Protective effect of HDACIs in improves survival and organ injury after CLP-induced sepsis [ Surg Open Sci, 2023, 12:35-42] PubMed: 36936452
Epigenetic alterations of CXCL5 in Cr(VI)-induced carcinogenesis [ Sci Total Environ, 2022, 838(Pt 1):155713] PubMed: 35660107
Targeting the MITF/APAF-1 axis as salvage therapy for MAPK inhibitors in resistant melanoma [ Cell Rep, 2022, 41(6):111601] PubMed: 36351409
Nicotinamide improves in vitro lens regeneration in a mouse capsular bag model [ Stem Cell Res Ther, 2022, 13(1):198] PubMed: 35550648
Effects of Hst3p inhibition in <i>Candida albicans</i>: a genome-wide H3K56 acetylation analysis [ Front Cell Infect Microbiol, 2022, 12:1031814] PubMed: 36389164
Nicotinamide n-Oxide Attenuates HSV-1-Induced Microglial Inflammation through Sirtuin-1/NF-κB Signaling [ Int J Mol Sci, 2022, 23(24)16085] PubMed: 36555725
Arylamine N-Acetyltransferase 1 Activity is Regulated by the Protein Acetylation Status [ Front Pharmacol, 2022, 13:797469] PubMed: 35153780
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] PubMed: 34508571
Naphthoquinone-induced arylation inhibits Sirtuin 7 activity [ J Cell Sci, 2022, jcs.259207] PubMed: 35319066

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.