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

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.

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SIRT6 activator 12q Chemical Structure

SIRT6 activator 12q Chemical Structure

CAS No. : 2601734-99-8

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Based on 1 publication(s) in Google Scholar

SIRT6 activator 12q Related Antibodies

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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

SIRT6

0.58 μM (EC1.5)

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].

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

SIRT6 activator 12q Related Antibodies

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]

MedChemExpress (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

Formula

C31H22N2O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2001 mL 11.0006 mL 22.0012 mL 55.0031 mL
5 mM 0.4400 mL 2.2001 mL 4.4002 mL 11.0006 mL
10 mM 0.2200 mL 1.1001 mL 2.2001 mL 5.5003 mL
15 mM 0.1467 mL 0.7334 mL 1.4667 mL 3.6669 mL
20 mM 0.1100 mL 0.5500 mL 1.1001 mL 2.7502 mL
25 mM 0.0880 mL 0.4400 mL 0.8800 mL 2.2001 mL
30 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8334 mL
40 mM 0.0550 mL 0.2750 mL 0.5500 mL 1.3751 mL
50 mM 0.0440 mL 0.2200 mL 0.4400 mL 1.1001 mL
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SIRT6 activator 12q Related Classifications

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.

Keywords:

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

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