Apostatin-1
Based on 1 publication(s) in Google Scholar
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin.
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- Pureza : 99.64%
- No. CAS: 2559703-06-7
- Fòrmula: C19H27N3OS
- Peso molecular:345.50
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Almacenamiento:Powder -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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Apostatin-1
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Actividad biológica
Descripciòn
IC50 & Target
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RIPK1 |
In Vitro
Apostatin-1 inhibits Velcade (Bortezomib, HY-134050)-induced apoptosis and RIPK1-dependent apoptosis (RDA) and necroptosis, with an IC50 of 0.97 μM[1].
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Apostatin-1 (10 μM, 6 h) effectively induces autophagy and the degradation of long-lived proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y, HeLa, HT-29, and Jurkat cells
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Concentration:10 μM
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Incubation Time:6 h
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Result:Effectively induced autophagy by LC3 II induction and p62 reduction.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type mice (n = 10, male, 8 weeks of age, systemic inflammation mouse model)[1]
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Dosage:20 mg/kg
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Administration:IP, once
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Result:Reduced expression of the TNF-induced inflammatory target gene products, NOS and COXII27, and of inflammatory cytokines in cells stimulated with pathogen-associated molecular patterns, including interferon γ (IFNγ), lipopolysaccharide (LPS), Pam3CSK4 (a synthetic bacterial lipopeptide), and muramyl dipeptide (MDP). Showed increased survival following intravenous delivery of TNF, a mouse model of systemic inflammation.
Chemical Information
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No. CAS 2559703-06-7
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Appearance Solid
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Peso molecular 345.50
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Fòrmula C19H27N3OS
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Color White to off-white
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SMILES
O=C(NC1CCCCCC1)C(SC2=NCCN2C)C3=CC=CC=C3
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Synonyms
Apt-1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci China Life Sci
Downregulation of METTL3 enhances TRADD-mediated apoptosis in inflammatory bowel disease. [Abstract]2025 Jul;68(7):2010-2027. PMID: 40347213
Solvente y solubilidad
In Vitro:
DMSO : 83.33 mg/mL (241.19 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C; 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)
In Vivo:
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: ≥ 2.5 mg/mL (7.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (277 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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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 |
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| DMSO | 1 mM | 2.8944 mL | 14.4718 mL | 28.9436 mL | 72.3589 mL |
| 5 mM | 0.5789 mL | 2.8944 mL | 5.7887 mL | 14.4718 mL | |
| 10 mM | 0.2894 mL | 1.4472 mL | 2.8944 mL | 7.2359 mL | |
| 15 mM | 0.1930 mL | 0.9648 mL | 1.9296 mL | 4.8239 mL | |
| 20 mM | 0.1447 mL | 0.7236 mL | 1.4472 mL | 3.6179 mL | |
| 25 mM | 0.1158 mL | 0.5789 mL | 1.1577 mL | 2.8944 mL | |
| 30 mM | 0.0965 mL | 0.4824 mL | 0.9648 mL | 2.4120 mL | |
| 40 mM | 0.0724 mL | 0.3618 mL | 0.7236 mL | 1.8090 mL | |
| 50 mM | 0.0579 mL | 0.2894 mL | 0.5789 mL | 1.4472 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 1.2060 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3618 mL | 0.9045 mL | |
| 100 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7236 mL |
Apostatin-1 Related Classifications
HY-134050 Related Classifications
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