2601734-99-8

2601734-99-8 structure
2601734-99-8 structure
  • Name: SIRT6 activator 12q
  • Chemical Name: SIRT6 activator 12q
  • CAS Number: 2601734-99-8
  • Molecular Formula: C31H22N2O2
  • Molecular Weight: 454.53
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2023-04-02 17:45:23
  • Modify Date: 2024-04-05 08:33:15
  • SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 µM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity[1].

Name SIRT6 activator 12q
Description SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 µM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity[1].
Related Catalog
Target

SIRT1:171.2 μM (IC50)

SIRT2:>200 μM (IC50)

SIRT3:>200 μM (IC50)

SIRT5:>200 μM (IC50)

SIRT6:0.58 μM (IC50)

In Vitro SIRT6 activator 12q (2.5, 5, 10 µM; 14, 18 days) 以剂量依赖性方式抑制 PANC-1、BXPC-3、MIAPaCa-2 和 AsPC-1 细胞的集落形成[1] . SIRT6 activator 12q (10, 25, 50 µM; 48 h) 以剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 G2 期[1]。 SIRT6 activator 12q (12.5, 25, 50 µM; 48 h) 以剂量依赖性方式降低 PANC-1 和 BXPC-3 细胞中 H3K9ac、H3K18ac 和 H3K56ac 的蛋白表达[1]。 Cell Viability Assay[1] Cell Line: PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells Concentration: 0-100 µM Incubation Time: 72 h Result: Showed antiproliferative activity with IC50s of 4.43, 8.27, 7.10, 9.66 µM for PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells, respectively. Cell Cycle Analysis[1] Cell Line: PANC-1, BXPC-3 cells Concentration: 10, 25, 50 µM Incubation Time: 48 h Result: Induced cell cycle arrest at G2 phase in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: PANC-1, BXPC-3 cells Concentration: 10, 25, 50 µM Incubation Time: 48 h Result: Induced apoptosis by increased Annexin V+ populations in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: PANC-1, BXPC-3 cells Concentration: 12.5, 25, 50 µM Incubation Time: 72 h Result: Decreased the protein levels of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner.
In Vivo SIRT6 activator 12q (100, 150 mg/kg; p.o.; daily for 30 days) 以剂量依赖性方式抑制小鼠肿瘤生长[1]。 Animal Model: BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-1)[1] Dosage: 100, 150 mg/kg Administration: P.o.; daily for 30 days Result: Inhibited tumer growth in a dose-dependent manner, and a tumor inhibition rate of 90.25% at a dose of 150 mg/kg.
References

[1]. Chen X, et al. Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity. J Med Chem. 2020 Sep 24;63(18):10474-10495.  

Molecular Formula C31H22N2O2
Molecular Weight 454.53