PBA-1105
Based on 1 Customer Validation
PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates.
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- Pureza: 99.47%
- No. CAS: 2410081-56-8
- Fòrmula: C39H48N2O6
- Peso molecular:640.81
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
PBA-1105 induces autophagic degradation of stably expressed mutant tau at DC50 of 0.71 nM and Dmax,24 hr of 100 nM, followed by a hook effect at higher concentrations[1].
PBA-1105 (0.1-10 μM; 24 hours) induces the autophagic degradation of misfolded proteins and aggregates at nanomolar concentrations. PBA-1105 leads to significant degradation of mutant tau and misfolded proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:1 μM
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Incubation Time:24 hours
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Result:Activated p62 oligomerization and increased autophagic flux of ubiquitinated aggregates.
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Cell Line:SH-SY5Y-tauP301L cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:24 hours
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Result:Selectively degraded mutant tauP301L with a DC50 of 0.71 nM and persistently cleared insoluble tau aggregates.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hTauP301L-BiFC transgenic mice[1]
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Dosage:20 or 50 mg/kg (PBS containing 30% polyethylene glycol (PEG))
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Administration:Intraperitoneal injection; three times per week; for 4 weeks
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Result:Effectively cleared tau aggregates in a dose-dependent manner, significantly reducing insoluble tau species in the brain while leaving soluble tau species unaffected.
Resulted in increased levels of autophagic markers like LC3, confirming the activation of autophagic degradation pathways.
Immunohistochemical analysis showed a marked reduction in tau oligomers and phosphorylated tau in both cortical and hippocampal regions.
Chemical Information
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No. CAS 2410081-56-8
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Appearance Liquid (Density: 1.129±0.06 g/cm3)
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Peso molecular 640.81
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Fòrmula C39H48N2O6
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Color Colorless to light yellow
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SMILES
O=C(CCCC1=CC=CC=C1)NCCOCCOCCOCCNCC2=CC(OCC3=CC=CC=C3)=C(OCC4=CC=CC=C4)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (156.05 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)
Pureza y Documentación
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Ficha de datos (269 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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.5605 mL | 7.8026 mL | 15.6052 mL | 39.0131 mL |
| 5 mM | 0.3121 mL | 1.5605 mL | 3.1210 mL | 7.8026 mL | |
| 10 mM | 0.1561 mL | 0.7803 mL | 1.5605 mL | 3.9013 mL | |
| 15 mM | 0.1040 mL | 0.5202 mL | 1.0403 mL | 2.6009 mL | |
| 20 mM | 0.0780 mL | 0.3901 mL | 0.7803 mL | 1.9507 mL | |
| 25 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5605 mL | |
| 30 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3004 mL | |
| 40 mM | 0.0390 mL | 0.1951 mL | 0.3901 mL | 0.9753 mL | |
| 50 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL | |
| 60 mM | 0.0260 mL | 0.1300 mL | 0.2601 mL | 0.6502 mL | |
| 80 mM | 0.0195 mL | 0.0975 mL | 0.1951 mL | 0.4877 mL | |
| 100 mM | 0.0156 mL | 0.0780 mL | 0.1561 mL | 0.3901 mL |
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