SIRT1-IN-2

SIRT1-IN-2 (compound 3h) is a potent and selective SIRT1 (silent information regulator 1) inhibitor, with an IC50 of 1.6 μM[1].

Signaling Pathways >> Epigenetics >> Sirtuin

Research Areas >> Cancer

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

SIRT1:1.6 μM (IC50)

SIRT2:39 μM (IC50)

SIRT1-IN-2 (compound 3h) (0-100 μM, 48 h) inhibits the proliferation of Human cancer cell lines including K562, HCT-116, HepG2, A549, and MCF-7, and shows significantly less cytotoxic on 293T cells 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, HepG2, A549, and MCF-7, with IC50 values of 51, 37, 40, 48, and 48 μM, respectively. And showed significantly less cytotoxic on 293T cells and HUVEC, with IC50 values of > 100 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.