S130
Based on 1 Customer Validation
S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 µM. S130 suppresses autophagy flux.
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- Pureza: 99.43%
- No. CAS: 1160852-22-1
- Fòrmula: C24H25N3O2
- Peso molecular:387.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
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Actividad biológica
IC50: 3.24 µM (ATG4B)[1]
S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity[1].
S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage[1].
S130 accumulates autolysosomes with more lipidated LC3[1].
S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis[1].
Nutrient deprivation enhances S130-induced cytotoxicity[1].
S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 µM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells, HCT116 cells, HL60 cells
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Concentration:0 μM, 3.1 μM, 6.3 μM, 12.5 μM, 25 μM
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Incubation Time:48 hours
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Result:Had significant cytotoxic effects on HeLa cells (IC50 =16.1 µM), HCT116 cells(IC50 =9.0 µM) and HL60 cells (IC50 =4.7 µM) at a dose higher than 6.3 µM. And such cytotoxicity might not cause cell death through necroptosis.
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Cell Line:HeLa cells and MEF cells
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Concentration:10 μM
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Incubation Time:6 hours
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Result:Suppressed autophagy at the early LC3 priming step or late autolysosome degradation stage.
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Cell Line:HeLa cells
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Concentration:0 μM, 5 μM, 10 μM
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Incubation Time:24 hours
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Result:Suppressed approximately 79% of the cleavage of full-length LC3-GST at 10 µM, while no substrates were processed in ATG4B KO cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude female mice (4 weeks), with HCT116 cells xenograft[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection; daily; 3 weeks
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Result:Was able to suppress tumor growth and with a sound safety on vital organs.
Chemical Information
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No. CAS 1160852-22-1
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Appearance Solid
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Peso molecular 387.47
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Fòrmula C24H25N3O2
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Color White to off-white
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SMILES
O=C1C2=CC=CC=C2C3=C4C1=NC=C(C(NCCCN(CC)CC)=O)C4=CC=C3
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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 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 125 mg/mL (322.61 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.25 mg/mL (5.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (5.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
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 (275 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5808 mL | 12.9042 mL | 25.8084 mL | 64.5211 mL |
| 5 mM | 0.5162 mL | 2.5808 mL | 5.1617 mL | 12.9042 mL | |
| 10 mM | 0.2581 mL | 1.2904 mL | 2.5808 mL | 6.4521 mL | |
| 15 mM | 0.1721 mL | 0.8603 mL | 1.7206 mL | 4.3014 mL | |
| 20 mM | 0.1290 mL | 0.6452 mL | 1.2904 mL | 3.2261 mL | |
| 25 mM | 0.1032 mL | 0.5162 mL | 1.0323 mL | 2.5808 mL | |
| 30 mM | 0.0860 mL | 0.4301 mL | 0.8603 mL | 2.1507 mL | |
| 40 mM | 0.0645 mL | 0.3226 mL | 0.6452 mL | 1.6130 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2904 mL | |
| 60 mM | 0.0430 mL | 0.2151 mL | 0.4301 mL | 1.0754 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8065 mL | |
| 100 mM | 0.0258 mL | 0.1290 mL | 0.2581 mL | 0.6452 mL |
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