SIRT6 activator 12q
Based on 1 Customer Validation
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.
- Purity: 99.83%
- CAS No.: 2601734-99-8
- Formula: C31H22N2O2
- Molecular Weight:454.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Antioxidant Compound Library
HY-L037
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Oxygen Sensing Compound Library
HY-L045
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Orally Active Compound Library
HY-L061
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Glutamine Metabolism Compound Library
HY-L064
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Radioprotector Library
HY-L178
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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SIRT6 0.58 μM (EC1.5) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | IC50 |
9.66 μM
Compound: 12q
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Antiproliferative activity against human AsPC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human AsPC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 32787077] |
| BXPC-3 | IC50 |
8.27 μM
Compound: 12q
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Antiproliferative activity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 32787077] |
| MIA PaCa-2 | IC50 |
7.1 μM
Compound: 12q
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Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 32787077] |
| PANC-1 | IC50 |
4.13 μM
Compound: 12q
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Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 32787077] |
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.
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Cell Line:PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells
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Concentration:0-100 µM
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Incubation Time:72 h
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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.
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Cell Line:PANC-1, BXPC-3 cells
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Concentration:10, 25, 50 µM
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Incubation Time:48 h
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Result:Induced cell cycle arrest at G2 phase in a dose-dependent manner.
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Cell Line:PANC-1, BXPC-3 cells
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Concentration:10, 25, 50 µM
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Incubation Time:48 h
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Result:Induced apoptosis by increased Annexin V+ populations in a concentration-dependent manner.
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Cell Line:PANC-1, BXPC-3 cells
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Concentration:12.5, 25, 50 µM
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Incubation Time:72 h
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Result:Decreased the protein levels of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner.
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-1)[1]
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Dosage:100, 150 mg/kg
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Administration:P.o.; daily for 30 days
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Result:Inhibited tumer growth in a dose-dependent manner, and a tumor inhibition rate of 90.25% at a dose of 150 mg/kg.
Chemical Information
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CAS No. 2601734-99-8
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Appearance Solid
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Molecular Weight 454.52
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Formula C31H22N2O2
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Color Off-white to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (285 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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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