Free shipping on all orders over $ 500

Sirtinol

Cat. No. M3010
Sirtinol Structure
Size Price Availability Quantity
5mg USD 60 In stock
25mg USD 210 In stock
100mg USD 600 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 394.47
Formula C26H22N2O2
CAS Number 410536-97-9
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
Related Sirtuin Products
Thiomyristoyl

Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.

Nicotinamide

Nicotinamide is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

Fisetin

Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.

Resveratrol

Resveratrol is a phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects.

SRT1720 Hydrochloride

SRT1720 Hydrochloride is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Sirtinol supplier, Sirtuin, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.