| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
SIRT1 171.2 μM (IC50) SIRT2 >200 μM (IC50) SIRT3 >200 μM (IC50) SIRT5 >200 μM (IC50) SIRT6 0.58 μM (IC50)
SIRT6 activator 12q targets SIRT6, an NAD+-dependent deacetylase involved in DNA repair, energy metabolism, aging regulation, and inflammation suppression. It demonstrates IC₅0 values of 171.20 microM for SIRT1, >200 microM for SIRT2, SIRT3, and SIRT5, and 0.58 microM for SIRT6, indicating high specificity. |
|---|---|
| ln Vitro |
SIRT6 activator 12q (10, 25, 50 µM; 48 h) promotes apoptosis and cell cycle arrest in the G2 phase in a dose-dependent manner [1]. SIRT6 activator 12q (2.5, 5, 10 µM; 14, 18 days) suppresses colony formation of PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells. In PANC-1 and BXPC-3 cells, SIRT6 activator 12q (12.5, 25, 50 µM; 48 h) dose-dependently decreases the protein expression of H3K9ac, H3K18ac, and H3K56ac [1].
In vitro, SIRT6 activator 12q inhibits the proliferation and migration of pancreatic ductal adenocarcinoma (PDAC) cells. It induces apoptosis and causes cell cycle arrest at the G2 phase. The compound activates SIRT6 deacetylase activity, leading to downstream effects on gene expression and cellular function. |
| ln Vivo |
In mice, SIRT6 activator 12q (100, 150 mg/kg; po; daily for 30 days) dose-dependently suppresses tumor growth [1].
In vivo, SIRT6 activator 12q markedly suppresses tumor growth in a PDAC tumor xenograft model. The compound is orally active, making it suitable for convenient administration. It displays anti-cancer activity and has potential therapeutic applications in cancer biology. |
| Enzyme Assay |
Enzyme assays for SIRT6 activator 12q measure SIRT6 deacetylase activity using purified enzyme and a fluorogenic peptide substrate. The compound is incubated with SIRT6, NAD+, and the substrate, and deacetylation is quantified by fluorescence. IC₅0 values for various sirtuin isoforms are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells Tested Concentrations: 0-100 µM Incubation Duration: 72 h Experimental Results: demonstrated 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 Types: PANC-1, BXPC-3 cells Tested Concentrations: 10, 25, 50 µM Incubation Duration: 48 h Experimental Results: Induced cell cycle arrest at G2 phase in a dose-dependent manner. Apoptosis Analysis[1] Cell Types: PANC-1, BXPC-3 cells Tested Concentrations: 10, 25, 50 µM Incubation Duration: 48 h Experimental Results: Induced apoptosis by increased Annexin V+ populations in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: PANC-1, BXPC-3 cells Tested Concentrations: 12.5, 25, 50 µM Incubation Duration: 72 h Experimental Results: diminished the protein levels of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner. Cellular assays for SIRT6 activator 12q utilize cancer cell lines such as PDAC cells. Cells are treated with the compound, and cell proliferation, migration, and apoptosis are assessed. SIRT6 activity and downstream target gene expression are measured by Western blot or qPCR. |
| Animal Protocol |
Animal/Disease Models: BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-1)[1]
Doses: 100, 150 mg/kg Route of Administration: Po; daily for 30 days Experimental Results: Inhibited tumor growth in a dose-dependent manner, and a tumor inhibition rate of 90.25% at a dose of 150 mg/kg. In vivo studies with SIRT6 activator 12q are conducted in mouse xenograft models. The compound is administered orally, and tumor growth is monitored. Pharmacodynamic markers such as SIRT6 activity and target gene expression are assessed in tumor tissues. |
| ADME/Pharmacokinetics |
SIRT6 activator 12q is orally active. It is soluble in DMSO and should be stored as a powder at -20degC. Standard pharmacokinetic studies would involve measuring plasma concentrations after oral administration to calculate parameters such as half-life, Cmax, and bioavailability.
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| Toxicity/Toxicokinetics |
Toxicity data for SIRT6 activator 12q are limited. The compound is a research tool and has not been extensively studied for toxicity. Standard safety precautions for laboratory handling of research compounds should be followed.
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| References | |
| Additional Infomation |
SIRT6 activator 12q is a research-use compound and is not approved for therapeutic applications. It is a selective SIRT6 activator used to study the role of SIRT6 in cancer, aging, and metabolism. The compound is available from multiple research suppliers with purity ≥98%.
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| Molecular Formula |
C31H22N2O2
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|---|---|
| Molecular Weight |
454.518587589264
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| Exact Mass |
454.168
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| CAS # |
2601734-99-8
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| PubChem CID |
156013743
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| Appearance |
Off-white to yellow solid powder
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| LogP |
6.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
682
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1=CC(C2OC3=CC=CC=C3C=2)=NC2C=CC=CC1=2)(=O)NC(C1C=CC=CC=1)C1C=CC=CC=1
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| InChi Key |
JNULQPRWYHVXHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H22N2O2/c34-31(33-30(21-11-3-1-4-12-21)22-13-5-2-6-14-22)25-20-27(32-26-17-9-8-16-24(25)26)29-19-23-15-7-10-18-28(23)35-29/h1-20,30H,(H,33,34)
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| Chemical Name |
N-benzhydryl-2-(1-benzofuran-2-yl)quinoline-4-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 25 mg/mL (55.00 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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