PKCβ inhibitor 1
Based on 1 publication(s) in Google Scholar
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.40%
- No. CAS: 257879-35-9
- Fòrmula: C24H21N5O2
- Peso molecular:411.46
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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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Publications Citing Use of MedChemExpress (MCE) PKCβ inhibitor 1
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Actividad biológica
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human PKCβ1 21 nM (IC50) |
human PKCβ2 5 nM (IC50) |
PKCα 331 nM (IC50) |
PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner[2].
PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells[2].
PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells[2].
PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells[2].
PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:2F7, BCBL-1 cells
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Concentration:0, 5, 10, 20, and 30 μM
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Incubation Time:48 hours
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Result:A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration.
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Cell Line:2F7 cells
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Concentration:14 μM
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Incubation Time:2-48 hours
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Result:Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment.
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Cell Line:BCBL-1 Cells
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Concentration:15 μM (the IC50)
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Incubation Time:2-48 hours
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Result:Inhibits cell cycle progression in 2F7 and BCBL-1 cells.
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Cell Line:BCBL-1 and 2F7 cell lines
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Concentration:15 or 14 μM (at the IC50 respectively)
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Incubation Time:2-48 hours
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Result:The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced.
Chemical Information
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No. CAS 257879-35-9
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Appearance Solid
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Peso molecular 411.46
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Fòrmula C24H21N5O2
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Color Yellow to orange
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SMILES
O=C(C(C1=CN(CCCN2C=CN=C2)C3=C1C=CC=C3)=C4NC5=CC=CC=C5)NC4=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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 250 mg/mL (607.59 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: ≥ 6.25 mg/mL (15.19 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.19 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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 (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tanaka M, et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4. [Content Brief]
[2]. Saba NS, et al. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J Investig Med. 2012 Jan;60(1):29-38. [Content Brief]
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 | 2.4304 mL | 12.1518 mL | 24.3037 mL | 60.7592 mL |
| 5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL | 12.1518 mL | |
| 10 mM | 0.2430 mL | 1.2152 mL | 2.4304 mL | 6.0759 mL | |
| 15 mM | 0.1620 mL | 0.8101 mL | 1.6202 mL | 4.0506 mL | |
| 20 mM | 0.1215 mL | 0.6076 mL | 1.2152 mL | 3.0380 mL | |
| 25 mM | 0.0972 mL | 0.4861 mL | 0.9721 mL | 2.4304 mL | |
| 30 mM | 0.0810 mL | 0.4051 mL | 0.8101 mL | 2.0253 mL | |
| 40 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5190 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4861 mL | 1.2152 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4051 mL | 1.0127 mL | |
| 80 mM | 0.0304 mL | 0.1519 mL | 0.3038 mL | 0.7595 mL | |
| 100 mM | 0.0243 mL | 0.1215 mL | 0.2430 mL | 0.6076 mL |
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