SKLB-11A
Based on 1 Customer Validation
SKLB-11A is a selective, orally active and allosteric SIRT3 (sirtuin 3) agonist with a Kd value of 4.7 μM. SKLB-11A is highly selective for other members of the SIRT family. SKLB-11A activates autophagy-related signaling pathways, prevents mitochondrial dysfunction, improves cardiac function in Doxorubicin (HY-15142A)-induced cardiotoxicity and myocardial ischemia/reperfusion models.
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- Pureté: 99.40%
- CAS No.: 433953-86-7
- Formule: C19H15FN4O2
- Masse moléculaire:350.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
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Epigenetics Compound Library
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Histone Modification Research Compound Library
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Autophagy Compound Library
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Anti-Aging Compound Library
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Antioxidant Compound Library
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Oxygen Sensing Compound Library
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Anti-Cardiovascular Disease Compound Library
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Orally Active Compound Library
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Glutamine Metabolism Compound Library
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Metabolic Enzyme Compound Library
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Highly Selective Activators Library
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Cell Death Library
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Radioprotector Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
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Cell Proliferation Compound Library
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High-Throughput Bioactive Compound Library
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Activité biologique
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SIRT3 4.7 μM (Kd) |
SKLB-11A enhances SIRT3 deacetylation activity with an EC50 of 21.95 μM[1].
SKLB-11A (0.625-5 μM; 24 h) does not alter SIRT3 protein levels but significantly enhances SIRT3 activity in H9c2 cells[1].
SKLB-11A binds to SIRT3 with high affinity and enhances its interaction with the p53-Ac substrate[1].
SKLB-11A (5-20 μM; 24 h) ameliorates Doxorubicin-induced mitochondrial damage and promotes SIRT3-mediated autophagy in H9c2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9c2 cells
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Concentration:0.625 μM, 1.25 μM, 2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Induced deacetylation at K122 and K68, resulting in enhanced MnSOD enzymatic activity.
Activated endogenous SIRT3 deacetylation in H9c2 cells.
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Cell Line:H9c2 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:24 h
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Result:Increased LC3-II expression and reduced p62 levels, indicating enhanced autophagic flux.
Increased the expression of PINK1 and Parkin, and promoted colocalization of mitochondria with Parkin and LC3-II.
SKLB-11A (20 mg/kg; oral gavage; daily; for 7 days) treatment alleviated ischemia/reperfusion (I/R)-induced myocardial injury in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (8 weeks, ~23 g)[1]
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Dosage:10 and 20 mg/kg/day
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Administration:Oral gavage; daily; for 7 days; then injected Doxorubicin intraperitoneally for 2 weeks
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Result:Significantly restored left ventricular ejection fraction (EF) and fractional shortening (FS) in a dose-dependent manner.
Partially reversed Doxorubicin-induced weight loss and reduced serum markers of myocardial injury, including LDH, CK-MB, and BNP.
Preserved myocardial structure and alleviated pathological damage.
Demonstrated no apparent toxicity at effective doses, as evidenced by preserved organ histology in the heart, liver, spleen, lungs, and kidneys.
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Animal Model:Male C57BL/6J mice (8-12 weeks old) was induced myocardial ischemia-reperfusion (I/R) injury[1].
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Dosage:20 mg/kg
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Administration:Oral gavage; daily; for 7 days
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Result:Restored cardiac function impaired by I/R injury.
Partially reversed I/R-induced elevations in serum myocardial injury markers, including LDH, CK-MB, and BNP.
Markedly reduced I/R-induced cardiac fibrosis.
Chemical Information
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CAS No. 433953-86-7
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Appearance Solid
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Masse moléculaire 350.35
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Formule C19H15FN4O2
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Color Light yellow to yellow
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SMILES
COC(C1=C(N)N(CC2=CC=C(F)C=C2)C3=NC4=CC=CC=C4N=C31)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 7.78 mg/mL (22.21 mM; Need ultrasonic; 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)
Pureté et documentation
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Fiche technique (280 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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Instruction de manipulation (2659 KB)
Références
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 | 2.8543 mL | 14.2714 mL | 28.5429 mL | 71.3572 mL |
| 5 mM | 0.5709 mL | 2.8543 mL | 5.7086 mL | 14.2714 mL | |
| 10 mM | 0.2854 mL | 1.4271 mL | 2.8543 mL | 7.1357 mL | |
| 15 mM | 0.1903 mL | 0.9514 mL | 1.9029 mL | 4.7571 mL | |
| 20 mM | 0.1427 mL | 0.7136 mL | 1.4271 mL | 3.5679 mL |
SKLB-11A Related Classifications
HY-173572 Related Classifications
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