CP21R7 |
رقم الكتالوجGC13176 |
CP21R7 هو مثبط قوي GSK-3β ، مع IC من 1.8 نانومتر ؛ يُظهر CP21R7 أيضًا نشاطًا مثبطًا ضد PKCα ، مع IC50 من 1900 نانومتر
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Cas No.: 125314-13-8
Sample solution is provided at 25 µL, 10mM.
CP21R7 is a potent and selective inhibitor of GSK3β.
The glycogen synthase kinase-3β (GSK-3β), a serine/threonine, is a ubiquitous kinase that participates in a multitude of cellular processes, such as cell membrane-to-nucleus signaling, gene transcription, translation, cytoskeletal structuring and cell cycle progression and survival [1].
In vitro: CP21R7 was an inhibitor of GSK3β and PKCα with the IC50 values of 1.8 and 1900 nM, respectively [1]. In the human reporter cell line, CP21R7 potently activated canonical Wnt signallingeven at the dose of 1 μM, with highest activity seen at 3 μM [2]. In human iPSCs exposed to N2B27 medium, supplemented with 1 μM GSK3β inhibitor CP21R7 strongly upregulated the expression of T (also known as Brachyury, T/BRY), a meso-endoderm marker expressed in the primitive streak [2].
References:
[1] Gong L, Hirschfeld D, Tan Y C, et al. Discovery of potent and bioavailable GSK-3β inhibitors[J]. Bioorganic & medicinal chemistry letters, 2010, 20(5): 1693-1696.
[2] Ciampi O, Iacone R, Longaretti L, et al. Generation of functional podocytes from human induced pluripotent stem cells[J]. Stem cell research, 2016, 17(1): 130-139.
Cas No. | 125314-13-8 | SDF | |
Chemical Name | 3-(3-aminophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione | ||
Canonical SMILES | NC1=CC=CC(C(C(N2)=O)=C(C3=CN(C)C4=C3C=CC=C4)C2=O)=C1 | ||
Formula | C19H15N3O2 | M.Wt | 317.3 |
الذوبان | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1516 mL | 15.758 mL | 31.5159 mL |
5 mM | 0.6303 mL | 3.1516 mL | 6.3032 mL |
10 mM | 0.3152 mL | 1.5758 mL | 3.1516 mL |
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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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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