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1-AzakenpaulloneGSK-3β inhibitor,potent and selective,cell-permeable

1-Azakenpaullone

Catalog No. BCC5332
Size Price Stock
2mg $130.00 In stock
5mg $237.00 In stock
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Quality Control of 1-Azakenpaullone

Chemical structure

1-Azakenpaullone

Biological Activity of 1-Azakenpaullone

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

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Chemical Properties of 1-Azakenpaullone

Cas No. 676596-65-9 SDF Download SDF
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)
Formula C15H10BrN3O M.Wt 328.16
Solubility Soluble in DMSO > 10 mM
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.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of 1-Azakenpaullone

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.

Background on 1-Azakenpaullone

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.

References on 1-Azakenpaullone

1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta.[Pubmed: 14698171]


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.

Kewords:

1-Azakenpaullone,676596-65-9,PI3K/Akt/mTOR Signaling,GSK-3, supplier, inhibitor,Antagonist,Blocker,Modulator,Agonist, activators, activates, potent, BioCrick

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