PKCβ inhibitor 1 (Synonyms: Protein Kinase Cβ Inhibitor) |
| رقم الكتالوجGC61995 |
PKCβ ؛ المانع 1 هو PKCβ قوي ، منافس ATP وانتقائي ؛ مثبط مع IC50s من 21 و 5 نانومتر للبشر PKCβ ؛ 1 و PKCβ ؛ 2 ، على التوالي. PKCβ ؛ يعرض المانع 1 انتقائية أكثر من 60 ضعفًا لصالح PKCβ ؛ 2 بالنسبة إلى نظائر PKC الأخرى (PKCα ؛، PKCγ ؛، و PKCε ؛).
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Cas No.: 257879-35-9
Sample solution is provided at 25 µL, 10mM.
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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)[1][2].
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].
[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.
[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.
| Cas No. | 257879-35-9 | SDF | |
| المرادفات | Protein Kinase Cβ Inhibitor | ||
| Canonical SMILES | O=C(C(C1=CN(CCCN2C=CN=C2)C3=C1C=CC=C3)=C4NC5=CC=CC=C5)NC4=O | ||
| Formula | C24H21N5O2 | M.Wt | 411.46 |
| الذوبان | DMSO : 250 mg/mL (607.59 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4304 mL | 12.1518 mL | 24.3037 mL |
| 5 mM | 0.4861 mL | 2.4304 mL | 4.8607 mL |
| 10 mM | 0.243 mL | 1.2152 mL | 2.4304 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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