Description: |
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.[1]. |
Target: |
SIRT7:325 nM (IC50) |
In Vivo: |
SIRT7 inhibitor 97491 (2 mg/kg; intraperitoneally injected; for 3 weeks, except on weekends) inhibits tumor growth in xenograft mice[1]. Animal Model: Balb/c nude mice (18-20 g; 6-8 weeks old) with MES-SA cells[1] Dosage: 2 mg/kg Administration: Intraperitoneally injected; for 3 weeks, except on weekends. Result: Inhibited cancer growth in vivo. |
In Vitro: |
SIRT7 inhibitor 97491 (1-10 μM) reduces cell growth in MES-SA cells, without causing cytotoxicity in HEK293 cells[1]. Cell Proliferation Assay[1] Cell Line: Human uterine sarcoma MES-SA cells Concentration: 1, 5, 10 μM Incubation Time: 72 hours Result: Led to more than 50% decrease in cell proliferation at concentrations of 5 and 10 μM. Cell Cytotoxicity Assay[1] Cell Line: Human embryonic kidney cell line HEK293 cells Concentration: 1, 5, 10 μM Incubation Time: 24 hours Result: HEK293 cells were almost unaffected. |
References: |
[1]. Ji-Hye Kim, et al. Identification of a Novel SIRT7 Inhibitor as Anticancer Drug Candidate. Biochem Biophys Res Commun. 2019 Jan 8;508(2):451-457. |