ICL-SIRT078

ICL-SIRT078 (0.5-25 µM; up to 15 days) inhibits the clonogenic proliferation of MCF-7 cells, with a significant reduction in colony formation at 12.5 and 25 µM^[1].

ICL-SIRT078 is highly selective for SIRT2 at up to 100 µM (> 65-fold selectivity over SIRT1, 3, and 5) and shows no measurable redox activity at 100 µM^[1].

ICL-SIRT078 (compound 10) (1.45 µM) inhibits human SIRT2 in the fluorescent p53 peptide assay, and the resynthesized material has an IC₅₀ of 1.45 µM^[1].
ICL-SIRT078 (0.17 µM) inhibits SIRT2 in the enzyme-coupled SIRT-Glo assay with an IC₅₀ of 0.17 µM and > 50-fold selectivity over SIRT1^[1].
ICL-SIRT078 has an IC₅₀ value of 3.96 µM as determined by fluorescence assay^[1].
ICL-SIRT078 (1.25-5 µM; 1 h) is a substrate-competitive SIRT2 inhibitor with a K_i of 0.62 µM that blocks the acetyl-lysine binding site, with no or minimal overlap with the NAD⁺ pocket^[1].
ICL-SIRT078 (1.45-10 µM; 48 h) exerts neuroprotective effects on N27 dopaminergic neurons exposed to Lactacystin (HY-16594), producing 23% neuroprotection at 1.45 µM and neurotoxicity at 10 µM and above^[1].
ICL-SIRT078 (1-10 μM; 10 min) inhibits SIRT2 with an IC₅₀ of 1.45 μM and > 100-fold selectivity over SIRT1, SIRT3, and SIRT5^[2].
ICL-SIRT078 (compound 19a) inhibits SIRT2 in the enzyme-coupled SIRT-Glo assay with an IC₅₀ of 0.17 μM^[2].
ICL-SIRT078 binds with a K value of 0.62 μM in the tubulin-K40 peptide competition assay^[2].
ICL-SIRT078 (20-50 μM; 24 h) induces α-tubulin hyperacetylation in MCF-7 cells^[2].
ICL-SIRT078 (compound 37) (1.4 µM) inhibits SIRT2 in an in vitro fluorescence assay using a p53-derived acetylated peptide substrate, with an IC₅₀ of 1.4 µM and > 50-fold isoform selectivity^[3].