Molecular Weight(MW): 394.47
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
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SIRT1 is involved in GABA-mediated protection against apoptosis and induction of insulin secretion. INS-1 cells are protected from apoptosis induced by tacrolimus (FK506; panel A) or streptozotocin (STZ, panel B) by GABA, and the protective effect is reversed by EX527 (SIRT1 inhibitor) or sirtinol (SIRT1 and SIRT2 inhibitor). The cells were incubated with GABA (100 uM), EX527 (200 nM) or sirtinol (4 uM) as indicated, for 1 h before adding 1 uM FK506, and cell viability was tested after 48 h. Similarly, STZ (2 mM) was added after the cells were incubated with other reagents for 1 h, but was replaced with the original medium containing all additives and no STZ after 1 h incubation. Viable cells were counted after 24 h. The results are representative of two experiments.
Biochem Biophys Res Commun 2014 452(3), 649-54. Sirtinol purchased from Selleck.
Effects of sirtinol on SIRT1 expression and HIF-1α. hMSCs were treated with sirtinol (100 uM) or equivalent concentration of DMSO (CTR) for 24 h and then exposed to 1% O2 for 6 h. All cells lysates were analyzed for SIRT1, HIF-1α, and tubulin by Western blot.
Biomed Res Int 2014 783459. Sirtinol purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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.|
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.  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.  Inhibition of Sirt1 by Sirtinol enhances UV- and H2O2-induced p53 acetylation to enhance cell death in cultured skin keratinocytes.  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. 
|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. |
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.
-  Grozinger CM, et al. J Biol Chem, 2001, 276(42), 38837-38843.
-  Mai A, et al. J Med Chem, 2005, 48(24), 7789-7795.
-  Ota H, et al. Oncogene, 2006, 25(2), 176-185.
-  Liu FC, et al. Acta Anaesthesiol Scand, 2008, 52(5), 635-640.
-  Kojima K, et al. Biochem Biophys Res Commun, 2008, 373(3), 423-428.
-  Cao C, et al. J Cell Mol Med, 2009, 13(9B), 3632-3643.
-  Jung-Hynes B, et al. J Biol Chem, 2009, 284(6), 3823-3832.
-  Sun JY, et al. Clin Lymphoma Myeloma Leuk, 2011, 11(1), 152-156.
|In vitro||DMSO||23 mg/mL (58.3 mM)|
|In vivo||2% DMSO+30% PEG 300+5% Tween 80+ddH2O||0.4mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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