Selisistat (EX 527) is a potent and selective inhibitor of the SIRT1 class III histone deacetylase enzyme. EX 527 has been used a powerful tool for studying the relationship between SIRT1 and cell regulation. The deacetylation of cortactin, a protein responsible for rearrangements of the actin cytoskeleton, is associated with cell motility and possibly tumorigenesis, and blocking of this deacetylation by EX 527 correlated to a decrease in cell motility. Blocking of SIRT1 by EX 527 also demonstrated that deacetylation of the important tumor suppressor protein p53 is mediated by SIRT1 as well.
Mol Neurobiol. 2018 Apr;55(4):3067-3078.
17β-Estradiol via SIRT1/Acetyl-p53/NF-kB Signaling Pathway Rescued Postnatal Rat Brain Against Acute Ethanol Intoxication
Selisistat (EX 527) purchased from AbMole
Free Radic Biol Med. 2018 Oct 17.
Resveratrol protects photoreceptors by blocking caspase- and PARP-dependent cell death pathways.
Selisistat (EX 527) purchased from AbMole
Cell Experiment | |
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Cell lines | NCI-H460 cells, MCF-7 cells, U-2 OS cells, or HMEC cell lines |
Preparation method | Cell viability assay. NCI-H460 cells, MCF-7 cells, U-2 OS cells, or HMEC were plated at 2,000 cells per well in opaque-walled 96-well plates (Corning) for the viability assay and 800 cells per well in 96-well Cytostar-T scintillating microplates (Amersham) for the proliferation assay. Cells were incubated for 1 day (NCI-H460) or 2 days (MCF-7, U-2 OS, and HMEC) prior to exposure to DNA-damaging agents and deacetylase inhibitors. All experiments were performed in triplicate.For viability assays, cells were treated with the indicated compounds for 48 h. Cell viability was then determined using the Cell Titer-Glo luminescent assay (Promega), which measures total ATP levels as an index of cell number. Luminescence was measured on a Luminoskan Ascent (ThermoLabSystems). |
Concentrations | 0~100 μM |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | Male Sprague-Dawley rats (8 weeks old, 200–250 g) and C57/B6 mice (8 weeks old) model |
Formulation | DMSO |
Dosages | 5-10 μg in a total volume of 5 μL |
Administration | Intracerebroventricular administration |
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.
Molecular Weight | 248.71 |
Formula | C13H13ClN2O |
CAS Number | 49843-98-3 |
Purity | 99.42% |
Solubility | DMSO 25 mg/mL |
Storage | at -20°C |
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