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Selisistat (EX 527)

Cat. No. M1708
Selisistat (EX 527) Structure
Synonym:

SEN0014196; Selisistat

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 48.6  USD54 In stock
5mg USD 45  USD50 In stock
10mg USD 59.4  USD66 In stock
50mg USD 135  USD150 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source Free Radical Biology and Medicine (2018). Figure 4. Ex-527 (Abmole Bioscience, Houston, TX, USA)
Method western blot
Cell Lines 661W cells
Concentrations 180 μM
Incubation Time
Results As shown in Figure 4A–D, there is a lower cell death rate in the presence of RSV in both the GD and the light exposure groups compared to the control group, whereas treatment with Ex-527 reversed this trend (P < 0.01).
Source Proc Natl Acad Sci U S A (2013). Figure 3. EX 527
Method Continuous Deacetylation Assay
Cell Lines Sir2Tm crystals
Concentrations 1 mM
Incubation Time 80 min
Results Ex-527 showed negligible affinities (Sir2Tm: Kd > 180 μM; Sirt3 Kd > 330 μM) to apo-enzymes and to the Sirtuins saturated with 1 mM peptide substrate (Sir2Tm: Kd > 170 μM; Sirt3: Kd > 180 μM).
Source Proc Natl Acad Sci U S A (2013). Figure 1. EX 527
Method Activity assay
Cell Lines Sir2Tm crystals
Concentrations 1.5 mM
Incubation Time 80 min
Results Activity assays in presence of varying Ex-527 concentrations showed that inhibition of Sir2Tm and Sirt3 by Ex-527 is noncompetitive with substrate peptide (Fig. 1 E and F; Fig. S1A; Sir2Tm Ki = 1.8 ± 0.4 μM, Sirt3 Ki = 33.4 ± 4.4 μM).
Protocol
Cell Experiment
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
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
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 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.

Chemical Information
Molecular Weight 248.71
Formula C13H13ClN2O
CAS Number 49843-98-3
Purity 99.42%
Solubility DMSO 25 mg/mL
Storage at -20°C
References

Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice
Xianfeng Wang, et al. Obesity (Silver Spring). 2015 Jun;23(6):1209-17. PMID: 25959124.

Activating transcription factor 4 confers a multidrug resistance phenotype to gastric cancer cells through transactivation of SIRT1 expression.
Zhu et al. PLoS One. 2012;7(2):e31431. PMID: 22363646.

The central Sirtuin 1/p53 pathway is essential for the orexigenic action of ghrelin.
Velásquez DA, et al. Diabetes. 2011 Apr;60(4):1177-85. PMID: 21386086.

Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage.
Solomon JM, et al. Mol Cell Biol. 2006 Jan;26(1):28-38. PMID: 16354677.

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Keywords: Selisistat (EX 527), SEN0014196; Selisistat supplier, HDAC, inhibitors

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