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Sirtinol

Catalog No.S2804

For research use only.

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

Sirtinol Chemical Structure

CAS No. 410536-97-9

Selleck's Sirtinol has been cited by 34 publications

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Sirtuin Signaling Pathways

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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 M4TKO3Bzd2yrZnXyZZRqd25iYYPzZZk> Mlz3N|Ah|ryP M1;5T|I1NTd{IHi= MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYYSgN|AhfU1iYX\0[ZIhOjRidH:gO|IhcHK| M4rkW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{SwNVY6Lz5{NEO0NFE3QTxxYU6=
human MCF7 cells NXrKZVRtTnWwY4Tpc44h[XO|YYm= M16wT|UxKM7:TR?= MUKyOEBp MorrTY5pcWKrdHnvckBw\iCVSWLUNUBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIFk\XS7bHH0bY9vKG:oIIC1N{BifCCueYOgN|gzKGG2IEWwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NUf6SFNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOFAyPjlpPkK0N|QxOTZ7PD;hQi=>
human U937 cells NX7re2N{SXCxcITvd4l{KGG|c3H5 NITCSFE2OCEQvF2= MWW0OUBp Mkf4TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCXOUO3JINmdGy|IHH0JFUxKHWPIHHmeIVzKDR3IHjyd{BjgSCobH;3JIN6fG:vZYTyfS=> M4OxXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MUi5PVY4Lz5{M{G4PVk3PzxxYU6=
Hs683 MonnRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmrZO|IhcHK| Ml3aRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKc{[4N{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTN|LkpOwG0> MoW2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2N{WzN|AoRjJ6NEe1N|MxRC:jPh?=
U373 NITkNo1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NUjZcXBEPzJiaILz MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV|N{OgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0{QS5|zszN Mn7oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2N{WzN|AoRjJ6NEe1N|MxRC:jPh?=
Hs683 MnX5R4VtdCCleXPs[UBie3OjeR?= MkfBNlQhfG9iNEigbJJ{ NIXa[pNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJezZ6MzDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgTWM2OCCjZoTldkAzPCC2bzC0PEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobH;3JIN6fG:vZYTyfS=> M{LLfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEe1N|MxLz5{OES3OVM{ODxxYU6=
Hs683 NX7tTIxoS2WubDDjfYNt\SCjc4PhfS=> MWmyOEB1dyB2ODDodpM> NUC3e3VrS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUHN4OEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZZQhUUN3MDDh[pRmeiB{NDD0c{A1QCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcI94KGO7dH;t[ZRzgQ>? NX3Qc2FGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0O|U{OzBpPkK4OFc2OzNyPD;hQi=>
U373 M2[5W2NmdGxiY4njcIUh[XO|YYm= NVXOdm9GOjRidH:gOFghcHK| MWnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDVN|c{KGOnbHzzJIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEBIOi:PIIDoZZNmKGG2IFnDOVAh[W[2ZYKgNlQhfG9iNEigbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2com= MoLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2N{WzN|AoRjJ6NEe1N|MxRC:jPh?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index 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 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 (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 Research:

[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 Research:

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

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

Chemical Information

Molecular Weight 394.47
Formula

C26H22N2O2
CAS No. 410536-97-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)NC(=O)C2=CC=CC=C2N=CC3=C(C=CC4=CC=CC=C43)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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.

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