Anle138b-F105
Based on 1 Customer Validation
Anle138b-F105 is an autophagy-targeting chimera (AUTOTAC) that targets p62/Sequestosome-1/SQSTM1. Anle138b-F105 binds to the ZZ domain of p62, induces conformational activation, self-oligomerization, interaction with LC3, and formation of autophagosomes. Anle138b-F105 induces autophagic flux of ubiquitin-conjugated aggregated proteins, leading to their lysosomal degradation. Anle138b-F105 is applicable for the research of neurodegenerative proteinopathies.
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- Pureté: 98.18%
- CAS No.: 2941386-44-1
- Formule: C36H37FN4O5
- Masse moléculaire:624.70
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Anle138b-F105 (1 mM; 2 h) induces p62 self-polymerization in HEK293T cells[1].
Anle138b-F105 (1 μM; 24 h) enhances autophagic turnover of Ub-conjugated protein aggregates in HEK293T cells, with an autophagic flux index of 2.6[1].
Anle138b-F105 (1 μM; 24 h) promotes sequestration of Ub-conjugated protein aggregates with p62 in HeLa cells[1].
Anle138b-F105 (0.001-10 μM; 24 h) selectively degrades aggregation-prone tauP301L in SH-SY5Y-tauP301L cells with a DC50 of 2.63 nM, and exhibits sustained degradative efficacy post-washout[1].
Anle138b-F105 (24 h) selectively degrades nuclear-localized mutant huntingtin (HttQ97-NLS-GFP) in HeLa cells with a DC50 of ~3 nM[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 mM
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Incubation Time:2 h
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Result:Induced the conversion of p62 monomers into oligomers and 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 h
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Result:Dose-dependently reduced tauP301L levels, with a half-degrading concentration (DC50) of 2.63 nM.
Achieved maximal degradation at 10 μM, and exhibited sustained efficacy for at least 8 h post-washout.
Chemical Information
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CAS No. 2941386-44-1
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Appearance Oil
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Masse moléculaire 624.70
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Formule C36H37FN4O5
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Color Off-white to light brown
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SMILES
FC(C=C1)=CC=C1COC2=CC=CC(CNCCOCCOCCNC3=CC(C4=CC(C5=CC=C(OCO6)C6=C5)=NN4)=CC=C3)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (160.08 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.00 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.6008 mL | 8.0038 mL | 16.0077 mL | 40.0192 mL |
| 5 mM | 0.3202 mL | 1.6008 mL | 3.2015 mL | 8.0038 mL | |
| 10 mM | 0.1601 mL | 0.8004 mL | 1.6008 mL | 4.0019 mL | |
| 15 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6679 mL | |
| 20 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0010 mL | |
| 25 mM | 0.0640 mL | 0.3202 mL | 0.6403 mL | 1.6008 mL | |
| 30 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3340 mL | |
| 40 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL | |
| 50 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8004 mL | |
| 60 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 80 mM | 0.0200 mL | 0.1000 mL | 0.2001 mL | 0.5002 mL | |
| 100 mM | 0.0160 mL | 0.0800 mL | 0.1601 mL | 0.4002 mL |