Home Epigenetics Sirtuin inhibitor Sirtinol For research use only.

Sirtinol

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

Sirtinol Chemical Structure

Sirtinol Chemical Structure

CAS No. 410536-97-9

Purity & Quality Control

Sirtinol Related Products

Signaling Pathway

Sirtuin Signaling Pathways

Sirtuin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells Proliferation assay 30 μM 24-72 h Antiproliferative activity against human MCF7 cells at 30 uM after 24 to 72 hrs 24340169
human MCF7 cells Function assay 50 μM 24 h Inhibition of SIRT1 in human MCF7 cells assessed as increase in acetylation of p53 at lys 382 at 50 uM after 24 hrs by Western blot analysis 24340169
human U937 cells Apoptosis assay 50 μM 45 h Induction of apoptosis in human U937 cells at 50 uM after 45 hrs by flow cytometry 23189967
Hs683 Antiproliferative assay 72 hrs Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay, IC50=33.9μM 28475330
U373 Antiproliferative assay 72 hrs Antiproliferative activity against human U373 cells after 72 hrs by MTT assay, IC50=39.3μM 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at G1 phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
U373 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human U373 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
Click to View More Cell Line Experimental Data

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
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]
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.
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 25184156
Western blot SIRT1 / p-AKT / Foxo3a / β-catenin Foxp3 / RORγt Ac-H3K9 / Fibrobectin / Collagen 1 / α-SMA 25184156
In Vivo
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]
Animal Research Animal Models Male Sprague-Dawley rats subjected to trauma-hemorrhage
Dosages 1 mg/kg
Administration Administered intravenously

Chemical Information & Solubility

Molecular Weight 394.47 Formula

C26H22N2O2
CAS No. 410536-97-9 SDF Download Sirtinol SDF
Smiles CC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2N=CC3=C(C=CC4=CC=CC=C43)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 23 mg/mL ( (58.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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