Selisistat (EX 527)

Catalog No.S1541 Synonyms: SEN0014196

Selisistat (EX 527) Chemical Structure

Molecular Weight(MW): 248.71

Selisistat (EX 527) is a potent and selective SIRT1 inhibitor with IC50 of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.

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In DMSO USD 46 In stock
USD 50 In stock
USD 80 In stock
USD 170 In stock
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5 Customer Reviews

  • The eect of Melatonin, luzindole, and EX527 treatment on apoptotic index, infarct size, lactate dehydrogenase (LDH) release, and CK release in IR-injured hearts. Representative photomicrographs of in situ detection of apoptotic myocytes by TUNEL staining. Green fluorescence shows TUNEL-positive nuclei; blue fluorescence shows nuclei of total cardiomyocytes; original magnification 9x400. Sacle bar: 100 um.

    J Pineal Res 2014 57(2), 228-38. Selisistat (EX 527) purchased from Selleck.

    Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT.

    Cancer Res 2014 74(1), 298-308. Selisistat (EX 527) purchased from Selleck.

  • (A) The fluorescence spectra of the HAT assay responsive to increasing concentrations of p300 (from bottom to top: 0, 0.05, 0.1, 0.5, 1.0, 5.0, 10, 20, 40, 60, 80, 100, 100, 120, 160, 200 and 400 nM) and (B) its calibration curve. (C) The fluorescence spectra of the HAT assay in response to the absence (black line) and presence (red line) of 60 μM p300 inhibitor C646. (D) Various concentrations of C646 were used for p300 inhibition. From top to bottom ([C646]: 0, 0.1, 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10, 20, 40 and 60 μM). Inset in (D) shows the fluorescence signal curve as a function of the concentration of C646. [p300]=120 nM. (For interpretation of the references to color in this figure legend, the reader is referred to the web version of this article.)

    Biosens Bioelectron, 2017, 91:400-407. Selisistat (EX 527) purchased from Selleck.

    EX-527 decreases bone marrow atrophy significantly in the lethal septic model (H & E; original magnification, x 40). Tissue samples of long bones (femur and tibia) were harvested at 48 hours after CLP. Samples were processed and stained with H & E, and representative images were chosen from different experimental groups. Semiquantitative pathology scores for bone marrow atrophy were graded according to the diameter proportion of veins to bone marrow cells (mean T SEM, n = 5-6 animals per group).

    J Trauma Acute Care Surg 2014 10.1097/TA.0347. Selisistat (EX 527) purchased from Selleck.

  • Western blot analysis of acetylated-lysine in Ex-527-treated embryos. Embryos were treated at the 2-cell stage with 100 and 200 umol/L of Ex-527, and extracts were collected 12 h later. Predictable band size of p53 is 53 kDa.

    Dev Growth Differ 2014 56(6), 460-8. Selisistat (EX 527) purchased from Selleck.

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Biological Activity

Description Selisistat (EX 527) is a potent and selective SIRT1 inhibitor with IC50 of 38 nM in a cell-free assay, exhibits >200-fold selectivity against SIRT2 and SIRT3. Phase 2.
Features Greater potency, specificity, stability, and lower toxicity than other inhibitors of SIRT1 catalytic activity identified to date.
Targets
SIRT1 [1]
(Cell-free assay)
38 nM
In vitro

EX 527 exhibits potently inhibitory effect against SIRT1 deacetylase activity in a concentration-dependent manner with an IC50 of 38 nM, displays much lower activity against SIRT2 and SIRT3 with IC50 values of 19.6 μM and 48.7 μM, respectively. EX 527 does not inhibit SIRT4-7 and class I/II HDAC activity at concentrations up to 100 μM. EX-527 alone (1 μM) has no detectable effect on the acetylation of p53 lysine 382 in NCI-H460 cells. EX-527 significantly increases the amount of acetylated p53 in NCI-H460 cells, human mammary epithelial cells, U-2 OS and MCF-7 cells subjected to genotoxic agents such as Etoposide, Doxorubicin, Hydroxyurea, and Hydrogen peroxide, which is more effective than that caused by Nicotinamide (5 mM). But surprisingly EX 527 does not result in detectable effects on p53-controled gene expression, cell survival, or cell proliferation. [1] EX 527 causes a 90% increase in cell number of HCT116 cells after 7 days in the condition of 0.1% serum but not 10% serum, suggesting that SIRT1 is a significant regulator of cell proliferation during growth factor deprivation conditions. [2] EX 527 abrogates resveratrol effects on glucose responses, and prevents resveratrol-induced up-regulation of Glut2, glucokinase, Pdx-1, and Tfam in INS-1E Cells, due to the opposite effect of EX 527 and resveratrol on SIRT1 deacetylase activity. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Platelets NV3mbmtuSXCxcITvd4l{KEG|c3H5 MkjVNVAwPTBizszN Mln5NVAhdWmw NYHq[FV{TE2VTx?= M2j6eolv[3KnYYPld{BTV1NibHX2[YwhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHfD[3YzPTh{OUS5OS=>
HEK 293 MmLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXUXHYzPCCq NIH4WY9KSzVyPUm3MlchyrFiOD6xJO69VQ>? M4DUd|I1QTl6NEK3
HeLa MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TK[FI1KGh? NIHHUVFKSzVyPUO3MlnDqMLzwrCxMlgh|ryP NFnEVmgzPDl7OESyOy=>
HEK 293 M360N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHOzeZA1QCCq NIW1cnFKSzVyPU[5MlDDqMLzwrCwMlch|ryP MlL1NlQ6QTh2Mke=
HeLa MkHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ETFN5PDhiaB?= NFS0ZVBKSzVyPUiuPeKhyrIEoEGuPUDPxE1? NVzKN3J[OjR7OUi0Nlc>
RMECs MX3BdI9xfG:|aYOgRZN{[Xl? Mnf6NVDDqM7:TR?= NUe1e49OOjUEoHi= MVXheJRmdnWjdHXzJJRp\SCjboTpMYFxd3C2b4TpZ{Bm\m[nY4Sgc4YhTGW|LVe= NUfUVmRrOjR2OE[xOFc>
HUVECs MVfBdI9xfG:|aYOgRZN{[Xl? M1zDZVExyqEQvF2= MXWyOEBp NYi0bnVv[m:uaYPo[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2IH;mJJJme3[ncnH0do9tKGmwIHPlcIwhfmmjYnnsbZR6 M1L0S|I{OzV6OUK4
K562 MUPGeY5kfGmxbjDBd5NigQ>? Mn;KNE4yNTFizszN NWL6[pJROiCq M3XLXJN1cW23bHH0[ZMhVnKoMj3k[ZBmdmSnboSg[4Vv\SC2cnHud4NzcXC2aX;u NWjOe2tCOjFzOU[0PVc>
INS-1E Ml:wSpVv[3Srb36gRZN{[Xl? NXrubYhHOSEQvH2= NESyUIkzPCCq MXXwdoV3\W62czDy[ZN3\XKjdILvcE1qdmS3Y3XkJJVxNXKnZ4XsZZRqd25ib3dCpGdtfXR{LDDncJVkd2urbnHz[UxR\HhvMTygZY5lyqCWZnHt M1fhWVIyOTZ|OUS2
MCF-7  NFnCbG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYW5T4x7OC1zMECg{txO MVKyOE81QC95MjDo NIS2bmFFVVOR MY\y[ZBz\XO|ZYOgZ4VtdCCycn;sbYZmemG2aX;uJIF1KHSqZTDjc45k\W62cnH0bY9vKOLLpUGwNEDPxE1? MnXXNlA{PzF5MEm=
NCI-H460  MnjoSpVv[3Srb36gRZN{[Xl? MYmxJO69dQ>? M1fab|YhcA>? NHPKeZFFVVOR NGPXPHlxem:mdXPld{BiKGOxbnPlcpRz[XSrb36t[IVx\W6mZX70JIlv[3KnYYPlJIlvKHSqZTDhcY92dnRib3[gZYNmfHmuYYTl[EBxPTN? MkD1NVY{PTR4N{e=

... Click to View More Cell Line Experimental Data

In vivo Administration of EX 527 (~10 μg) to rats increases hypothalamic acetyl-p53 levels by inhibiting hypothalamic SIRT1 activity. Co-administration of EX 527 with ghrelin markedly blunts the orexigenic action of ghrelin by decreasing the pAMPK levels, increasing the ACC levels, and abolishing the higher expression of the transcription factors FoxO1, pCREB, and Bsx and the neuropeptides NPY and AgRP in the hypothalamic arcuate nucleus. [4]

Protocol

Kinase Assay:[1]
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Inhibition of GST-SIRT1 deacetylase activity:

293T cells are transiently transfected with GST-tagged human SIRT1 in the pDEST27 Gateway vector using FuGENE-6. After 48 hours, the cells are lysed with 50 mM Tris, pH 8.0, 120 mM NaCl, 1 mM EDTA, and 0.5% Nonidet P-40, supplemented with Complete Mini protease inhibitor cocktail tablets. GST-SIRT1 is purified from lysates using glutathione-Sepharose beads and washed extensively in the above buffer. The deacetylation assay is performed with approximately 30 ng of GST-SIRT1 in the presence of EX 527 (48 pM to 100 μM). Deacetylation is measured using the Fluor de Lys kit using a fluorogenic peptide encompassing residues 379 to 382 of p53, acetylated on lysine 382. The acetylated lysine residue is coupled to an aminomethylcoumarin moiety. The peptide is deacetylated by SIRT1, followed by the addition of a proteolytic developer that releases the fluorescent aminomethylcoumarin. Briefly, enzyme preparations are incubated with 170 μM NAD+ and 100 μM p53 fluorogenic peptide for 45 minutes at 37 °C followed by incubation in developer for 15 minutes at 37 °C. Fluorescence is measured by excitation at 360 nm and emission at 460 nm and enzymatic activity is expressed in relative fluorescence units.
Cell Research:[1]
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  • Cell lines: NCI-H460, MCF-7, U-2 OS and HMEC
  • Concentrations: Dissolved in DMSO, final concentration 1 μM
  • Incubation Time: 48 or 72 hours
  • Method: For viability assays, cells are treated with EX 527 for 48 hours. Cell viability is then determined using the Cell Titer-Glo luminescent assay, which measures total ATP level as an index of cell number. Luminescence is measured on a Luminoskan Ascent. For the proliferation assay, 0.5 μCi/mL of [14C]thymidine is added to the medium immediately after EX 527. Plates are counted at 48 hours (HMEC) or 72 hours (NCI-H460, MCF-7, and U-2 OS cells) in a Microbeta liquid scintillation counter. Thymidine incorporated by the cells is detected by proximity to the scintillant in the base of the Cytostar-T tissue culture plate.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Male Sprague-Dawley rats
  • Formulation: Dissolved in DMSO in a total volume of 5 μL
  • Dosages: ~5 μg/rat
  • Administration: Intracerebroventricular injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 49 mg/mL (197.01 mM)
Ethanol 18 mg/mL (72.37 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+30% PEG 300+ddH2O
15mg/mL

* 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.

Chemical Information

Molecular Weight 248.71
Formula

C13H13ClN2O

CAS No. 49843-98-3
Storage powder
Synonyms SEN0014196

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01485965 Completed Huntingtons Disease Siena Biotech S.p.A. November 2011 Phase 1
NCT01521585 Completed Huntingtons Disease Siena Biotech S.p.A. November 2011 Phase 2
NCT01485952 Completed Huntington Disease Siena Biotech S.p.A.|Seventh Framework Programme|European Huntingtons Disease Network March 2011 Phase 1
NCT01521832 Completed Huntingtons Disease Siena Biotech S.p.A. October 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    what is the extinction coefficient of S1541 WX527?

  • Answer:

    The extinction coefficient of S1541 EX-527 is 1421.650635.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID