SIRT1-IN-3

SIRT1-IN-3 (compound 3j) is a potent and selective SIRT1 inhibitor, with an IC50 of 4.2 μM[1].

Signaling Pathways >> Epigenetics >> Sirtuin

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Sirtuin

SIRT1:4.2 μM (IC50)

SIRT2:38 μM (IC50)

SIRT1-IN-3 (compound 3j) (0-100 μM, 48 h) inhibits the proliferation of human cancer cell lines including K562, HCT-116, H460, HepG2, A549, and MCF-7, and shows low cytotoxic on 293T and HUVEC[1]. Cell Cytotoxicity Assay Cell Line: Human cancer cell lines (K562, HCT-116, H460, HepG2, A549, HT-29, MCF-7) and normal cell lines (293T, HUVEC)[1] Concentration: 0, 0.01, 0.1, 1, 10, 100 μM Incubation Time: 48 h Result: Inhibited the proliferation of Human cancer cell lines including K562, HCT-116, H460, HepG2, A549, and MCF-7, with IC50 values of 47, 41, 66, 93, 52, and 64 μM, respectively. And showed low cytotoxic on 293T and HUVEC, with an IC50 values of 49 and 45 μM, respectively.

[1]. Laaroussi H, Ding Y, Teng Y, et al. Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents. Eur J Med Chem. 2020;202:112561.