2. Apoptosis
    Epigenetics
    Cell Cycle/DNA Damage
  3. Apoptosis
    Sirtuin
  4. SIRT6 activator 12q

SIRT6 activator 12q 

Cat. No.: HY-148712 Purity: 98.01%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

SIRT6 activator 12q Chemical Structure

SIRT6 activator 12q Chemical Structure

CAS No. : 2601734-99-8

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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].

IC50 & 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 (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[1].
SIRT6 activator 12q (10, 25, 50 µM; 48 h) induces apoptosis and cell cycle arrest at G2 phase in a dose-dependent manner[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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) inhibites the tumer growth in a dose-dependent manner in mouse[1].
Pharmacokinetic Parameters of SIRT6 activator 12q in Male Sprague-Dawley rats[1].

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
T1/2 (h) 7.52 ± 1.44 9.06 ± 0.21
Tmax (h) 2.00 ± 0.00 0.08 ± 0.00
Cmax (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[1]

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)[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.
Molecular Weight

454.52

Appearance

Solid

Formula

C31H22N2O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2001 mL 11.0006 mL 22.0012 mL
5 mM 0.4400 mL 2.2001 mL 4.4002 mL
10 mM 0.2200 mL 1.1001 mL 2.2001 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.75 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

SIRT6 activator 12q2601734-99-8ApoptosisSirtuinantiproliferationantimigrationapoptosisPANC-1BXPC-3 cellsanticancerInhibitorinhibitorinhibit

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