SIRT6-IN-3
Based on 1 Customer Validation
SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC50=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.
For research use only. We do not sell to patients.
- Purity: 98.19%
- CAS No.: 3023471-40-8
- Formula: C21H30Br3ClN6S
- Molecular Weight:673.73
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
|
SIRT1 80.52 μM (IC50) |
SIRT2 92.21 μM (IC50) |
SIRT6 7.46 μM (IC50) |
HDAC3 111.9 μM (IC50) |
HDAC6 96.77 μM (IC50) |
HDAC8 102 μM (IC50) |
SIRT6-IN-3 (25 μM, 48 h) induces PDAC cell-cycle arrest and apoptosis[1].
SIRT6-IN-3 (25 μM, 72 h) inhibits the proliferation of pancreatic cancer cells by inhibiting signaling pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PDAC cells
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Concentration:0, 6.25, 12.5, 25 μM
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Incubation Time:48 h
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Result:Increased the percentages of the G0-G1 phase and decreased cyclin D1 expression in a dose-dependent manner.
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Cell Line:PDAC cells
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Concentration:0, 6.25, 12.5, 25 μM
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Incubation Time:Overnight
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Result:Significantly down-regulated p-mTOR, p-P70S6K, p-AKT, and p-ERK.
Inhibited the activity of both mTORC1 and mTORC2.
Significantly up-regulated the expression of cleaved-PARP, cleaved-Caspase3, and cleaved-Caspase9.
SIRT6-IN-3 (HY-156027; 20 mg/kg for i.p; once every 2 days for 4 weeks) enhances the antitumor effects of gemcitabine in vivo when in combination with gemcitabine (ratio 2 : 1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tumor mouse model[1]
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Dosage:20 mg/kg (in combination with 10 mg/kg gemcitabine)
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Administration:Intraperitoneal injection (i.p.); Once every 2 days for 4 weeks
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Result:Inhibited the tumor mass 71.3% in mice with combinations of gemcitabine.
Greatly increased the expression of apoptosis maker.
Chemical Information
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CAS No. 3023471-40-8
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Appearance Solid
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Molecular Weight 673.73
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Formula C21H30Br3ClN6S
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Color Light yellow to yellow
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SMILES
BrC1=C(Br)NC(C2=NC=CC3=C2N=CN3CCCCCCS/C(N(C)C)=[N+](C)\C)=C1.Cl.[Br-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 120 mg/mL (178.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 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 (protect from light, stored under nitrogen). 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 | 1.4843 mL | 7.4214 mL | 14.8427 mL | 37.1069 mL |
| 5 mM | 0.2969 mL | 1.4843 mL | 2.9685 mL | 7.4214 mL | |
| 10 mM | 0.1484 mL | 0.7421 mL | 1.4843 mL | 3.7107 mL | |
| 15 mM | 0.0990 mL | 0.4948 mL | 0.9895 mL | 2.4738 mL | |
| 20 mM | 0.0742 mL | 0.3711 mL | 0.7421 mL | 1.8553 mL | |
| 25 mM | 0.0594 mL | 0.2969 mL | 0.5937 mL | 1.4843 mL | |
| 30 mM | 0.0495 mL | 0.2474 mL | 0.4948 mL | 1.2369 mL | |
| 40 mM | 0.0371 mL | 0.1855 mL | 0.3711 mL | 0.9277 mL | |
| 50 mM | 0.0297 mL | 0.1484 mL | 0.2969 mL | 0.7421 mL | |
| 60 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6184 mL | |
| 80 mM | 0.0186 mL | 0.0928 mL | 0.1855 mL | 0.4638 mL | |
| 100 mM | 0.0148 mL | 0.0742 mL | 0.1484 mL | 0.3711 mL |