Sirtinol

For research use only.

Catalog No.S2804

23 publications

Sirtinol Chemical Structure

CAS No. 410536-97-9

Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.

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Selleck's Sirtinol has been cited by 23 publications

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Biological Activity

Description Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
Features Sirtinol does not inhibit class I and class II HDACs.
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells NG[wPWtRem:uaX\ldoF1cW:wIHHzd4F6 M1HJUFMxKM7:TR?= M4LLWlI1NTd{IHi= MmTURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHH0JFMxKHWPIHHmeIVzKDJ2IITvJFczKGi{cx?= NXPPc|M6OjR|NECxOlk>
human MCF7 cells NIW2Z4lHfW6ldHnvckBie3OjeR?= M2HoNVUxKM7:TR?= NEHXSJYzPCCq MUTJcohq[mm2aX;uJI9nKFOLUmSxJIlvKGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZYNmfHmuYYTpc44hd2ZicEWzJIF1KGy7czCzPFIh[XRiNUCgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MYeyOFM1ODF4OR?=
human U937 cells Ml7nRZBweHSxc3nzJIF{e2G7 MYm1NEDPxE1? MVS0OUBp M2fC[Wlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iVUmzO{Bk\WyuczDheEA2OCC3TTDh[pRmeiB2NTDodpMh[nliZnzve{BkgXSxbXX0dpk> M1TsdFI{OTh7OU[3

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 25184156     


Effect of sirtinol on cellular proliferation of H1299 cells. H1299 cells treated with different concentrations (5, 10, 20 and 50 μM) of sirtinol for 24 h and 48 h, respectively. The cell survival was determined by the trypan blue staining assay combined with the Countess Automated Cell Counter. **P < 0.001 against vehicle control.

25184156
Western blot
SIRT1 / p-AKT / Foxo3a / β-catenin ; 

PubMed: 25184156     


Modulation of protein levels in NSCLC H1299 cells after sirtinol treatment. H1299 cells treated with indicated concentrations (10, 20, and 50 μM) of sirtinol for 24 h, respectively. The results of Western blot of Sirt1 nonhistone target protein, including FoxO3a, Akt phosphorylation, and β-catenin. β-Actin as an internal control.

Foxp3 / RORγt ; 

PubMed: 29090089     


The effect of sirtinol on the expressions of RORγt and Foxp3 measured by western blots. Shown are representative of five separate experiments.

Ac-H3K9 / Fibrobectin / Collagen 1 / α-SMA ; 

PubMed: 24833701     


Normally cultured NRK-49F cells were treated with sirtinol (0-50 μM) for 36 hours. Then, cell lysates were prepared and subjected to immunoblot analysis with antibodies for acetyl-H3K9 (Ac-H3K9), α-SMA, collagen I, fibronectin, or α-tubulin. Representative immunoblots from three or more experiments are shown.

25184156 29090089 24833701
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]

Protocol

Kinase Assay:

[1]
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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 Research:

[7]
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  • 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.


    (Only for Reference)
Animal Research:

[4]
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  • Animal Models: Male Sprague-Dawley rats subjected to trauma-hemorrhage
  • Dosages: 1 mg/kg
  • Administration: Administered intravenously
    (Only for Reference)

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(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		0.4mg/mL

* 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 Information

Molecular Weight 394.47
Formula

C26H22N2O2
CAS No. 410536-97-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2N=CC3=C(C=CC4=CC=CC=C43)O

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Sirtuin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID