SIRT2-IN-11

SIRT2-IN-11 (AEM1) is a selective SIRT2 inhibitor with an IC50 value of 18.5 μM. SIRT2-IN-11 p53-dependently induces apoptosis, activates expression of CDKN1A, PUMA and NOXA, and increases acetylation of p53. SIRT2-IN-11 can be used for the research of p53-related cancers[1].

Signaling Pathways >> Epigenetics >> Sirtuin

Research Areas >> Cancer

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

SIRT2:18.5 μM (IC50)

SIRT1:118.4 μM (IC50)

SIRT2-IN-11 (0-1000 μM) shows inhibitory effect of SIRT2-dependent deacetylation of MAL with an IC50 value of 18.5 μM[1]. SIRT2-IN-11 (0-1000 μM) weakly inhibits SIRT1 with an IC50 value of 118.4 μM[1]. SIRT2-IN-11 (0-20 μM; 8 h) induces cell apoptosis of lung cancer cells[1]. SIRT2-IN-11 (20 μM; 6 h) increases p53 acetylation and expression levels of Cp53 target genes CDKN1A, PUMA and NOXA[1]. RT-PCR[1] Cell Line: NSCLC cell lines Concentration: 20 μM Incubation Time: 6 hours Result: Increased the expression of CDKN1A, PUMA and NOXA. Apoptosis Analysis[1] Cell Line: A549 cell line Concentration: 0, 0.5, 1, 5, 10 and 20 μM Incubation Time: 24 hours Result: Mildly increased apoptosis of A549 cells, but when combined treatment with etoposide caused a marked increase in apoptosis.

[1]. Hoffmann G, et al. A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer. J Biol Chem. 2014 Feb 21;289(8):5208-16.