Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
COX-2/PI3K-IN-2 (compound 5f) is a potent PI3K inhibitor with IC50 value of 2.78 nM. COX-2/PI3K-IN-2 is a selective COX-2 inhibitor with Ki value of 3.02 nM. COX-2/PI3K-IN-2 shows anti-inflammatory and anti-cancer properties[1].