SIRT7 inhibitor 97491 is a potent SIRT 7 inhibitor that reduces the deacetylase activity of SIRT7 in a dose-dependent manner with an IC50 of 325 nM. SIRT7 inhibitor 97491 increases p53 stability through acetylation at K373/382. In addition, SIRT7 inhibitor 97491 promotes cell apoptosis through the caspase pathway[1].
In vitro, treatment with SIRT7 inhibitor 97491 (5 µM, 10 µM) for 72 hours resulted in a reduction of MES-SA cell proliferation by more than 50% without causing toxic effects on HEK 293 cells[1].
In vivo, three weeks of treatment with SIRT7 inhibitor 97491 (20 mg/kg/day; i.p.) inhibited tumor growth in xenograft mice[1].
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.
SIRT7 inhibitor 97491是一种有效的SIRT 7抑制剂,以剂量依赖性方式降低SIRT7的脱乙酰酶活性,IC50为325 nM。 SIRT7 inhibitor 97491通过在K373/382处乙酰化增加p53稳定性。此外,SIRT7 inhibitor 97491通过caspase途径促进细胞凋亡[1]。
在体外,SIRT7 inhibitor 97491(5µM 、10 µM)浓度处理72h导致MES-SA细胞增殖减少超过了50%,而不会对HEK 293细胞造成毒性影响[1]。
在体内,SIRT7 inhibitor 97491 (20mg/kg/day; i.p.) 治疗三周可以抑制异种移植小鼠的肿瘤生长[1]。