PP5-IN-1
Based on 1 Customer Validation
PP5-IN-1 is a competitive and selective serine/threonine protein phosphatase 5 (PP5) inhibitor with a Ki value of 244 nM. PP5-IN-1 induces extrinsic apoptosis (Apoptosis), disrupts the integrity of complex II, and activates Caspase 8. PP5-IN-1 can be used in research related to clear cell renal cell carcinoma.
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- Pureza: 99.47%
- No. CAS: 1022417-69-1
- Fòrmula: C18H18N2O3S
- Peso molecular:342.41
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Apoptosis Compound Library
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Ver todos los productos específicos de isoformas Caspase
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Actividad biológica
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Caspase 8 |
PP5-IN-1 (Compound P053) (100-1200 nM; 10 min) competitively inhibits recombinant PP5 protein with a Ki of 244 nM[1].
PP5-IN-1 (0-40 μM; 24 h) selectively inhibits proliferation of VHL-null ccRCC cell lines (786-O, A498) with dose-dependent efficacy, but does not significantly affect VHL-positive ccRCC cell lines (Caki-1, Caki-2) or normal renal HK2 cells[1].
PP5-IN-1 (10 μM; 24 h) induces extrinsic Apoptosis in 786-O VHL-null ccRCC cells, as evidenced by cleavage of caspase 8, caspase 3, and PARP, with no activation of the intrinsic apoptotic pathway marker caspase 9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VHL-null ccRCC cell lines (786-O, A498), VHL-positive ccRCC cell lines (Caki-1, Caki-2), normal renal epithelial cell line (HK2)
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Concentration:0, 10, 20, 30, 40 μM
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Incubation Time:24 h
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Result:Significantly inhibited proliferation of VHL-null ccRCC cell lines 786-O and A498 in a dose-dependent manner, with stronger effects at 30 and 40 μM.
Had no significant inhibitory effect on proliferation of VHL-positive ccRCC cell lines (Caki-1, Caki-2) or normal renal epithelial HK2 cells.
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Cell Line:786-O VHL-null ccRCC cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced cleavage of caspase 3, caspase 8, and poly-ADP ribose polymerase (PARP), hallmarks of apoptosis.
Showed no cleavage of caspase 9, indicating activation of the extrinsic apoptotic pathway.
Chemical Information
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No. CAS 1022417-69-1
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Appearance Solid
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Peso molecular 342.41
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Fòrmula C18H18N2O3S
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Color Yellow to orange
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SMILES
O=S(NC1=CC=C(CC2=CC=CC=C2)C=C1)(C3=C(C)ON=C3C)=O
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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
Solvente y solubilidad
DMSO : 100 mg/mL (292.05 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)
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 (7.30 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 (7.30 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.
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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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- 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9205 mL | 14.6024 mL | 29.2048 mL | 73.0119 mL |
| 5 mM | 0.5841 mL | 2.9205 mL | 5.8410 mL | 14.6024 mL | |
| 10 mM | 0.2920 mL | 1.4602 mL | 2.9205 mL | 7.3012 mL | |
| 15 mM | 0.1947 mL | 0.9735 mL | 1.9470 mL | 4.8675 mL | |
| 20 mM | 0.1460 mL | 0.7301 mL | 1.4602 mL | 3.6506 mL | |
| 25 mM | 0.1168 mL | 0.5841 mL | 1.1682 mL | 2.9205 mL | |
| 30 mM | 0.0973 mL | 0.4867 mL | 0.9735 mL | 2.4337 mL | |
| 40 mM | 0.0730 mL | 0.3651 mL | 0.7301 mL | 1.8253 mL | |
| 50 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4602 mL | |
| 60 mM | 0.0487 mL | 0.2434 mL | 0.4867 mL | 1.2169 mL | |
| 80 mM | 0.0365 mL | 0.1825 mL | 0.3651 mL | 0.9126 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7301 mL |
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