SIRT6 activator 12q - ≥98% , CAS No.2601734-99-8

CAS: 2601734-99-8 Cat. No.: S647275 Molecular Weight: 454.52

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

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 )

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

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 activ

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥98%

Names and Identifiers

• Canonical Smiles: O=C(C1=CC(C2=CC3=C(C=CC=C3)O2)=NC4=C1C=CC=C4)NC(C5=CC=CC=C5)C6=CC=CC=C6
• Molecular Weight: 454.52

Chemical and Physical Properties

• Solubility: DMSO : 25 mg/mL (55.00 mM; ultrasonic and warming and heat to 70°C)