EX 527 (Selisistat) 49843-98-3

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Molecular Weight:

248.71 EX 527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits >200-fold selectivity against SIRT2 and SIRT3.


Biological Activity


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.


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. 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.


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.

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Product Categories : Epigenetics > Sirtuin Inhibitor