1005095-06-6

1005095-06-6 structure
1005095-06-6 structure
  • Name: SIRT2-IN-11
  • Chemical Name: WAY-324197
  • CAS Number: 1005095-06-6
  • Molecular Formula: C21H22N2O
  • Molecular Weight: 318.4
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Sirtuin
  • Create Date: 2022-11-30 10:54:49
  • Modify Date: 2024-04-06 13:50:21
  • 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].

Name WAY-324197
Synonyms 7,10-Methanophenanthridine-2-carboxamide, 5,6,6a,7,8,9,10,10a-octahydro-6-phenyl-
Description 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].
Related Catalog
Target

SIRT2:18.5 μM (IC50)

SIRT1:118.4 μM (IC50)

In Vitro 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.
References

[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.  

Molecular Formula C21H22N2O
Molecular Weight 318.4