1. Cell Cycle/DNA Damage
    Epigenetics
  2. Sirtuin
  3. Selisistat

Selisistat (Synonyms: EX-527)

Cat. No.: HY-15452 Purity: 99.85%
Handling Instructions

Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.

For research use only. We do not sell to patients.

Selisistat Chemical Structure

Selisistat Chemical Structure

CAS No. : 49843-98-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 110 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of Selisistat:

Top Publications Citing Use of Products

    Selisistat purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 May 19;18(5). pii: E1063.

    Inhibition of sirt1 and AMPK blocked Rb2-induced hepatic autophagy. HepG2 cells are pretreated with 50 µM Rb2 for 4 h in the presence or absence of the sirt1 inhibitor EX-528 (EX) and the specific AMPK inhibitor Compound C (CC), and then subjected to OA (1 mM for HepG2 and 2 mM for primary mouse hepatocytes) exposure for 12 h. For lipid content determination, intracellular TG are stained by Oil red O (ORO). ORO is then eluted with isopropanol and the optical absorbance of the eluate is measured

    Selisistat purchased from MCE. Usage Cited in: Oncotarget. 2017 Apr 18;8(32):52783-52791.

    Immunoblot analysis of p-AKT (Ser473) and LC3-II in cells treated with 50 nM of TCO for 24 h in the presence and absence of EX-527.

    Selisistat purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 Mar 6;1863(6):595-603.

    LC3 deacetylation levels after erythropoietin (EPO) treatment are detected in PA-treated cells that have been treated with or without the SIRT1 inhibitor EX-527.

    Selisistat purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Aug 3;9:854.

    Western blotting and quantitative analysis of XBP-1 and ATF6 levels normalized to GAPDH in mice (n=6). Western blotting and quantitative analysis of P-Smad3 and ac-Smad3 levels normalized to T-Smad3 (n=6). I stands for ISO, G stands for GE, and E stands for Ex-527.

    Selisistat purchased from MCE. Usage Cited in: Metab Brain Dis. 2019 Feb;34(1):203-212.

    Western analysis of the protein expression of Sirt1, FoxO1 and LC3 protein in the PC12 with the treatment of MPP+, ECH and EX527.

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    Description

    Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.

    IC50 & Target[4]

    SIRT1

    98 nM (IC50)

    SIRT2

    19.6 μM (IC50)

    SIRT3

    48.7 μM (IC50)

    In Vitro

    Selisistat (EX-527) is an inhibitor of SIRT1 enzymatic activity (IC50, 98 nM), identified in a high-throughput screen using bacterially expressed human SIRT1. Selisistat (EX-527) inhibits SIRT1 in a concentration-dependent manner with an IC50 of 38 nM, in agreement with the activity on bacterially expressed SIRT1. Selisistat (EX-527) has much lower potency against SIRT2 (IC50, 19.6 μM) or SIRT3 (IC50, 48.7 μM) but does not inhibit class I/II HDAC activity at concentrations up to 100 μM[1]. Selisistat (EX-527) exerts an inhibitory effect on SIRT1 activity without affecting SIRT1 expression on both mRNA and protein levels[2].

    In Vivo

    Selisistat (EX-527) abolishes Resveratrol (RSV)-induced attenuation of microvascular inflammation in ob/ob septic mice. Finally, ob/ob mice in Sepsis+RSV group has significantly increased 7-day survival vs. Sepsis+Vehicle group[3].

    Clinical Trial
    Molecular Weight

    248.71

    Formula

    C₁₃H₁₃ClN₂O

    CAS No.

    49843-98-3

    SMILES

    O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (402.07 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0207 mL 20.1037 mL 40.2075 mL
    5 mM 0.8041 mL 4.0207 mL 8.0415 mL
    10 mM 0.4021 mL 2.0104 mL 4.0207 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (10.05 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    The immortal mouse macrophage cell line RAW264.7 are used. Cells are seeded in 96-well dishes at a density of 3 × 103 cells/cm2 and treated with high glucose at the concentrations of 5.6, 11.1, 25 and 30 mM, alone or with SRT1720 (1 μM) or Selisistat(10 μM) for 24 h. The stock solution of SRT1720 or Selisistat is prepared by dissolving each of them (in powder form) respectively in DMSO yielding a concentration of 100 μM and then stored at -80°C. MTT solution (0.5 mg/mL) is then added to each well and cells are incubated for 4 h at 37°C in a 5% CO2 incubator. Subsequently, the supernatant is removed, the formation of farmazan is solubilized with DMSO and measured at 540 nm with a Bio-Rad Model 680 Plate Reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3] Mice are injected with Resveratrol (RSV) 30mg/kg (4 mL/kg) or equivalent volume of DMSO (Vehicle) (4 mL/kg) intraperitoneally 18 hours pre-sepsis. This dose of RSV in mice is as per documented literature. In one group of mice, RSV pre-treated mice receive Selisistat (10 mg/kg intraperitoneally; 4mL/kg, Vehicle: DMSO) within 10 minutes of cecal ligation and puncture.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.85%

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    Keywords:

    SelisistatEX-527EX527EX 527SirtuinInhibitorinhibitorinhibit

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    Product name:
    Selisistat
    Cat. No.:
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