A homogeneous time-resolved fluorescence screen to identify SIRT2 deacetylase and defatty-acylase inhibitors
Fig 3
SIRT2 binding and inhibition of SIRT2 deacylase activities by 1.
(A) Displacement of Cy3-myristoyl-H4K16 peptide from SIRT2 by 1 as measured by a reduction in Cy3 fluorescence. The IC50 value of 16 μM was used to calculate a Kd of 5 μM for the interaction of 1 with SIRT2 (see Materials and Methods). (B) 1 inhibited SIRT2 deacetylase activity with an IC50 of 7 μM. (C) 1 inhibited SIRT2 de-decanoylase activity with an IC50 of 8 μM. (D) 1 inhibited SIRT2 de-dodecanoylase activity with an IC50 of 39 μM. (E) 1 inhibited SIRT2 demyristoylase activity with an IC50 of 37 μM. See Materials and Methods for assay conditions.