1-AzakenpaulloneGSK-3β inhibitor,potent and selective,cell-permeable CAS# 676596-65-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 676596-65-9 | SDF | Download SDF |
| PubChem ID | 6538897 | Appearance | Powder |
| Formula | C15H10BrN3O | M.Wt | 328.16 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 35.71 mg/mL (108.82 mM; Need ultrasonic) | ||
| SMILES | C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br | ||
| Standard InChIKey | NTSBZVCEIVPKBJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H10BrN3O/c16-8-3-4-11-9(6-8)10-7-13(20)18-12-2-1-5-17-15(12)14(10)19-11/h1-6,19H,7H2,(H,18,20) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 1-Azakenpaullone is a potent and selective inhibitor of GSK-3β with IC50 of 18 nM. | |||||
| Targets | GSK-3β | |||||
| IC50 | 18 nM | |||||
1-Azakenpaullone Dilution Calculator
1-Azakenpaullone Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0473 mL | 15.2365 mL | 30.4729 mL | 60.9459 mL | 76.1824 mL |
| 5 mM | 0.6095 mL | 3.0473 mL | 6.0946 mL | 12.1892 mL | 15.2365 mL |
| 10 mM | 0.3047 mL | 1.5236 mL | 3.0473 mL | 6.0946 mL | 7.6182 mL |
| 50 mM | 0.0609 mL | 0.3047 mL | 0.6095 mL | 1.2189 mL | 1.5236 mL |
| 100 mM | 0.0305 mL | 0.1524 mL | 0.3047 mL | 0.6095 mL | 0.7618 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.[Pubmed:14698171]
Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
Kenpaullone derivatives with a modified parent ring system were synthesized in order to develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1-Azakenpaullone was found to act as a selective GSK-3beta versus CDK1 inhibitor. The charge distribution within the 1-Azakenpaullone molecule is discussed as a possible explanation for the enhanced GSK-3beta selectivity of 1-Azakenpaullone compared to other paullone derivatives.
