Selisistat (EX 527)

For research use only.

Catalog No.S1541 Synonyms: SEN0014196

162 publications

Selisistat (EX 527) Chemical Structure

CAS No. 49843-98-3

Selisistat (EX 527, SEN0014196) 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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10mM (1mL in DMSO) RMB 647.01 In stock
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Selleck's Selisistat (EX 527) has been cited by 162 publications

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Description Selisistat (EX 527, SEN0014196) 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.
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 NGLiR3ZCeG:ydH;zbZMhSXO|YYm= NV33eo82OTBxNUCg{txO M2S0SlExKG2rbh?= M4PkU2ROW09? NX:zU45XcW6lcnXhd4V{KFKRUzDs[ZZmdCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYnDdWNGOjV6Mkm0PVU>
HEK 293 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzaNlQhcA>? NEThcopKSzVyPUm3MlchyrFiOD6xJO69VQ>? MX6yOFk6QDR{Nx?=
HeLa M4foemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:0WVI1KGh? NWW4Z3JvUUN3ME2zO{46yqEEsdMgNU45KM7:TR?= Mn7mNlQ6QTh2Mke=
HEK 293 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvpNnM1QCCq MV7JR|UxRTZ7LkFCpOKyyqByLkeg{txO MmTMNlQ6QTh2Mke=
HeLa NUj3clRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXmOFghcA>? NGrVToJKSzVyPUiuPeKhyrIEoEGuPUDPxE1? MlLwNlQ6QTh2Mke=
RMECs NVHYZ41DSXCxcITvd4l{KEG|c3H5 M3n4blExyqEQvF2= MUGyOOKhcA>? M2PVeYF1fGWwdXH0[ZMhfGinIHHueIku[XCxcITveIlkKGWoZnXjeEBw\iCGZYOtSy=> M1\jWlI1PDh4MUS3
HUVECs M1viRmFxd3C2b4Ppd{BCe3OjeR?= NGn2bJkyOMLizszN MoDPNlQhcA>? M1;RZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDy[ZN3\XKjdILvcEBqdiClZXzsJJZq[WKrbHn0fS=> M3rzRVI{OzV6OUK4
K562 NXjRTYZ{TnWwY4Tpc44hSXO|YYm= MWCwMlEuOSEQvF2= MXmyJIg> NIW0TJd{fGmvdXzheIV{KE6{ZkKt[IVx\W6mZX70JIdmdmVidILhcpNkemmydHnvci=> NV;qe2NTOjFzOU[0PVc>
INS-1E MX3GeY5kfGmxbjDBd5NigQ>? MlewNUDPxG1? NVzLeYwyOjRiaB?= MlK2dJJmfmWwdIOgdoV{fmW{YYTyc4wucW6mdXPl[EB2eC2{ZXf1cIF1cW:wIH;mxsBIdHW2Mjyg[4x2[2:taX7hd4UtWGS6LUGsJIFv\MLiVH\hcS=> MmjiNlEyPjN7NE[=
MCF-7  M2jzNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLoNE0yODBizszN MnjWNlQwPDhxN{KgbC=> M{DqSWROW09? NHHJNmxz\XC{ZYPz[ZMh[2WubDDwdo9tcW[ncnH0bY9vKGG2IITo[UBkd26lZX70doF1cW:wIPMJqVExOCEQvF2= NILTT5AzODN5MUewPS=>
NCI-H460  M1r5e2Z2dmO2aX;uJGF{e2G7 NGDKfpcyKM7:bR?= NVjwSHRNPiCq M1\zS2ROW09? MXrwdo9lfWOnczDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJJRp\SCjbX;1cpQhd2ZiYXPleJlt[XSnZDDwOVM> M1XOd|E3OzV2Nke3

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
GRP78 / FASL / Bcl-2 / LC3 ; 

PubMed: 29312612     

Western blot analysis of GRP78, FASL and LC3II after 0.5 mg/ml SB or 1 μM EX527 treatment of CL1-5 cells for 24 h. 

Ac-H3K9 / Fibronectin / Collagen 1 / α-SMA; 

PubMed: 24833701     

NRK-49F cells were treated with EX527 (0–100 μM) for 36 hours. Then, cell lysates were prepared and subjected to immunoblot analysis with antibodies for acetyl-H3K9 (Ac-H3K9), α-SMA, collagen I, fibronectin, or glyceraldehyde-3-phosphate dehydrogenase.

PCNA / Cyclin D1 / Cyclin E; 

PubMed: 24833701     

NRK-49F cells were cultured in medium with 5% fetal bovine serum and treated with EX527 (0–100 μM) for 36 hours. Then, cell lysates were prepared and subjected to immunoblot analysis with antibodies for PCNA, cyclin D1, cyclin E, or glyceraldehyde-3-phosp䲧疝Ỵ疞㧀疜膉痘 


PubMed: 24833701     

Cultured NRK-49F cells were treated with EX527 (0–100 μM) for 36 hours. Cell lysates were prepared and subjected to immunoblot analysis with antibodies for phospho-EGFR (pEGFR; Tyr1068), phospho-PDGFRβ (pPDGFRβ; Tyr751), EGFR, PDGFRβ, glyceraldehyde-3-pho䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖

pSTAT3 / STAT3 ; 

PubMed: 24833701     

NRK-49F cells were cultured in medium with 5% fetal bovine serum (FBS) and then treated with EX527 (0–100 μM) for 36 hours. After treatment, cell lysates were prepared and subjected to immunoblot analysis with antibodies for phospho-STAT3 (pSTAT3; Tyr705)䲧疝Ỵ疞㧀

p27 ; 

PubMed: 25143434     

A & B. SIRT1 inhibition with SIRT1 inhibitors upregulates p27 expression. H1299 (A) and H460 (B) cells were treated with Ex527 1 uM, Sirtinol 100 uM or Nicotinamide 10 mM for 12 hrs. Immunoblot analysis was performed with p27kip1 and β-actin antibodies.

FOXO3a / SIRT1 / Ac-p53 / p16(INK4a) ; 

PubMed: 31223423     

Whole cell lysates were subjected to western blot analysis for determining protein levels of FOXO3a, SIRT1, acetylated p53, p16INK4a, and p21 in senescent EPCs (endothelial progenitor cells). 

29312612 24833701 25143434 31223423

PubMed: 26824501     

M-P. Subcellular localization of hp-p38 in Bel-7402 (M-N) and SMMC-7721 (O-P) cells treated with identical amounts of either DMSO or EX527 at a final concentration of 50 μM for 24 h. Scale bar, 50 μm.

Growth inhibition assay
Cell viability ; 

PubMed: 24484175     

Growth inhibitory effect of EX527 on pancreatic cancer cell lines but not 293T cells. PANC-1, BXPC-3, ASPC-1, and 293T cells were exposed to different concentrations of EX527 for 48 h, and MTT assay was used to determine cell viability.

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]


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]
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  • Animal Models: Male Sprague-Dawley rats
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 49843-98-3
Storage powder
in solvent
Synonyms SEN0014196
Smiles C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

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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