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Sirtinol

Cat. No. M3010
Sirtinol Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 52  USD52 In stock
5mg USD 48  USD48 In stock
10mg USD 76  USD76 In stock
50mg USD 304  USD304 In stock
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Quality Control & Documentation
Biological Activity

Sirtinol is a specific NAD-dependant class III histone deacetylase sirtuin inhibitor targeting human Sirt1 and Sirt2 with IC50 of 131 μM and 38 μM, respectively. Sirtinol is slightly less potent against recombinant yeast Sir2p with IC50 of 68 μM. Sirtinol does not affect HDAC1 activity at 50 μM, suggesting that it specifically inhibits sirtuin deacetylase activity. Unlike TSA, Sirtinol treatment does not cause HeLa cells to change from a rounded morphology to a flattened morphology. Consistently, TSA causes robust acetylation of histones H3 and H4, as well as α-tubulin, whereas Sirtinol does not produce any of these effects. Treatment with Sirtinol inhibits body-axis formation and vascularization in Arabidopsis. Although Sirtinol (100 μM) has no axonal toxicity on uninjured axons, it effectively blocks NAD-dependent axonal protection (NDAP) after transection, indicating that Sirt1 proteins are likely effectors of this process. Sirtinol significantly increases mononucleosomes and oligonucleosomes in the cytoplasm of cardiac myocytes, a sensitive marker of apoptosis, and induces cleavage of caspase-3 almost equally as H2O2. [3] Sirtinol induces senescence-like growth arrest in human breast cancer MCF-7 cells and lung cancer H1299 cells, characterized by induction of senescence-associated β-galactosidase activity and increased expression of plasminogen activator inhibitor 1 Sirtinol-induced senescence-like growth arrest is accompanied by impaired activation of Ras-MAPK pathways but not Akt/PKB in response to epidermal growth factor (EGF) and insulin-like growth factor-I (IGF-I). Similar to Nicotinamide, Sirtinol inhibits the growth of MiaPaAa-2, BxPC-3, SOJ-6, and HeLa cells with IC50 of 48.1 μM, 48.5 μM, 48.4 μM, 53.9 μM, respectively.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines LNCaP, 22Rv1, DU145, and PC3
Preparation method Growing cell to 60% confluence and then treating them 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). Adding trypan blue (0.4% in PBS; 10 μL) to a smaller aliquot (10 μL) of cell suspension, and the number of cells (viable unstained and nonviable blue) are counted.
Concentrations Dissolved in DMSO, final concentrations ~120 μM
Incubation time 24 or 48 hours
Animal Experiment
Animal models Male Sprague-Dawley rats subjected to trauma-hemorrhage
Formulation Dissolved in DMSO, and diluted in saline
Dosages 1 mg/kg
Administration Administered intravenously
Chemical Information
Molecular Weight 394.47
Formula C26H22N2O2
CAS Number 410536-97-9
Solubility (25°C) DMSO 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Qing Ye, et al. Sirtinol regulates the balance of Th17/Treg to prevent allograft rejection

[2] Mingming Zhang, et al. Sirtinol promotes PEPCK1 degradation and inhibits gluconeogenesis by inhibiting deacetylase SIRT2

[3] Yung-Fong Tsai, et al. Sirtinol inhibits neutrophil elastase activity and attenuates lipopolysaccharide-mediated acute lung injury in mice

[4] Fu-Chao Liu, et al. Sirtinol attenuates trauma hemorrhage-induced hepatic injury through Akt-dependent pathway in rats

[5] Jos M Villalba, et al. Sirtuin activators and inhibitors

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