SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC 50 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 In Vitro SIRT6 activator 12q (compound12q) (2.5, 5, 10 µM; 14, 18 days) inhibits the colony formation of PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells in a dose-dependent manner. SIRT6 activator 12q (10, 25, 50 µM; 48 h) induces apoptosis and cell cycle arrest at G2 phase in a dose-dependent manner. SIRT6 activator 12q (12.5, 25, 50 µM; 48 h) decreases the protein expression of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells Concentration: 0-100 µM Incubation Time: 72 h Result: Showed antiproliferative activity with IC 50 s of 4.43, 8.27, 7.10, 9.66 µM for PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells, respectively. Cell Cycle AnalysisCell 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 AnalysisCell 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 AnalysisCell 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) inhibites the tumer growth in a dose-dependent manner in mouse . Pharmacokinetic Parameters of SIRT6 activator 12q in Male Sprague-Dawley rats . PK parameter 10 mg/kg p.o. 2 mg/kg i.v. CL (L/h/kg) 0.6 ± 0.08 Vss (L/kg) 1112.8 ± 322.84 T 1/2 (h) 7.52 ± 1.44 9.06 ± 0.21 T max (h) 2.00 ± 0.00 0.08 ± 0.00 C max (ng/mL) 98.45 ± 3.62 5123.70 ± 905.5 AUC (0-t) (h·ng/mL) 704.67 ± 80.47 3326.13 ± 476.4 AUC (0-∞) (h·ng/mL) 755.57 ± 80.74 3381.49 ± 468.48 F (%) 4.24 ± 0.48 Male Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-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. Form:Solid IC50& Target:SIRT1 171.2 μM (IC 50 ) SIRT2 >200 μM (IC 50 ) SIRT3 >200 μM (IC 50 ) SIRT5 >200 μM (IC 50 ) SIRT6 0.58 μM (IC 50 )