1-Azakenpaullone |
| رقم الكتالوجGC13907 |
1-Azakenpaullone (1-Akp) هو مثبط انتقائي للغاية وتنافسي ATP من glycogen synthase kinase-3 (GSK-3β) ، بقيمة IC50 تبلغ 18 نانومتر
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Cas No.: 676596-65-9
Sample solution is provided at 25 µL, 10mM.
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1-Azakenpaullone is a selective and cell-permeable inhibitor of glycogen synthase kinase-3β (GSK-3β) with IC50 value of 18nM [1, 2].
1-Azakenpaullone is a kenpaullone derivative with a modified heterocyclic basic structure. It shows potent inhibitory activity against GSK-3β over CDK1/cyclin B and CDK5/p25. The IC50 values for CDK1/cyclin B, CDK5/p25 and GSK-3β are 2μM, 4.2μM and 18nM, respectively. As an inhibitor of GSK-3β, 1-Azakenpaullone is developed as potential antidiabetic drug. 1-Azakenpaullone is found to protect rat insulinoma cell line INS-1E cells from glucolipotoxicity and stimulate cell proliferation. Besides that, 1-Azakenpaullone promotes the replication of beta cells in isolated rat islets at concentration of 1μM. In addition, 1-Azakenpaullone is reported to have effect in changing cardiac myocyte morphology. It increases cell area primarily through the elongation of the cells [1, 2 and 3].
References:
[1] Kunick C, Lauenroth K, Leost M, et al. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β. Bioorganic & medicinal chemistry letters, 2004, 14(2): 413-416.
[2] Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.
[3] Markou T, Cullingford T E, Giraldo A, et al. Glycogen synthase kinases 3α and 3β in cardiac myocytes: regulation and consequences of their inhibition. Cellular signalling, 2008, 20(1): 206-218.
| Cas No. | 676596-65-9 | SDF | |
| Canonical SMILES | C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br | ||
| Formula | C15H10BrN3O | M.Wt | 328.16 |
| الذوبان | ≥ 15.05mg/mL in DMSO | 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 | 3.0473 mL | 15.2365 mL | 30.4729 mL |
| 5 mM | 0.6095 mL | 3.0473 mL | 6.0946 mL |
| 10 mM | 0.3047 mL | 1.5236 mL | 3.0473 mL |
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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