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Sirtinol Sirtuin inhibitor

Cat.No.S2804

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

Chemical Structure

Molecular Weight: 394.47

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Quality Control

Cell Culture, Treatment & Working Concentration

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
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Chemical Information, Storage & Stability

Molecular Weight 394.47 Formula

C26H22N2O2

 Storage (From the date of receipt)
CAS No. 410536-97-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2N=CC3=C(C=CC4=CC=CC=C43)O

Solubility

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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Mechanism of Action

Features
Sirtinol does not inhibit class I and class II HDACs.
Targets/IC50/Ki
SIRT2 [1]
(Cell-free assay)
38 μM
SIRT1 [2]
(Cell-free assay)
131 μM
In vitro
Sirtinol potently inhibits recombinant yeast Sir2p activity in vitro with IC50 of 68 μM. Unlike TSA, this compound has shown no effect on human HDAC1, indicating that it is a selective sirtuin inhibitor. Unlike TSA, treatment of human primary fibroblasts with this chemical 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] Treatment with this inhibitor at 100 μM for 24 hours causes a sustained growth arrest in MCF-7 and H1299 cells for up to 9 days after its withdrawal. This treatment induces increased SA-β-gal activity and expression of PAI-1 in both MCF-7 and H1299 cells, more potently than Splitomicin. It inhibits colony formation at concentrations of 33 μM and higher in MCF-7 and H1299 cells, more effectively compared with Splitomicin. This compound (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. It 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 cells treated with this inhibitor. [3] Inhibition of Sirt1 by this chemical enhances UV- and H2O2-induced p53 acetylation to enhance cell death in cultured skin keratinocytes. [6] Blocking of Sirt1 by this 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.
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]
References
  • https://pubmed.ncbi.nlm.nih.gov/18419717/
  • https://pubmed.ncbi.nlm.nih.gov/18573234/
  • https://pubmed.ncbi.nlm.nih.gov/18681908/
  • https://pubmed.ncbi.nlm.nih.gov/19075016/
  • https://pubmed.ncbi.nlm.nih.gov/21454220/

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability S2804-viability1 25184156
Western blot SIRT1 / p-AKT / Foxo3a / β-catenin Foxp3 / RORγt Ac-H3K9 / Fibrobectin / Collagen 1 / α-SMA S2804-WB1 25184156

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