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1-Azakenpaullone

Catalog No. T6358   CAS 676596-65-9
Synonyms: azakenpaullone

1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, <100-fold selectivity over CDK1/cyclin B and CDK5/p25.

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1-Azakenpaullone Chemical Structure
1-Azakenpaullone, CAS 676596-65-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 72.00
2 mg In stock $ 101.00
5 mg In stock $ 198.00
10 mg In stock $ 328.00
25 mg In stock $ 590.00
50 mg In stock $ 843.00
100 mg In stock $ 1,150.00
500 mg In stock $ 2,290.00
1 mL * 10 mM (in DMSO) In stock $ 196.00
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Purity: 99.6%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 1-Azakenpaullone (azakenpaullone) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.
Targets&IC50 GSK-3β:18 nM
In vitro 1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. [1] In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. [2] 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. [3][4]
In vivo Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive de?cits, and improves the ketamine-induced motor incoordination in rotarod test. [5]
Kinase Assay Kinase preparations and assays: GSK-3β is assayed, following a 1/100 dilution in 1 mg BSA per mL 10 mM dithiothreitol, with 5 μL 40 μM GS-1 peptide as a substrate, in buffer A, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol-1; 1 mCi·mL-1 ) in a final volume of 30 μL. After 30 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto 2.5×3 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed five times in a solution of 10 mL phosphoric acid per L of water. The wet filters are counted in the presence of 1 mL ACS scintillation fluid. The kinase activity of CDK1/cyclin B is assayed in buffer C, with 1 mg/mL histone H1, in the presence of 15 μM [γ-32P]ATP (3000 Ci·mmol-1; 1 mCi·mL-1 ) in a final volume of 30 μL. After 10 min incubation at 30℃, 25 μL aliquots of supernatant are spotted onto P81 phosphocellulose papers and treated as described above. The activity of CDK5/p25 is assayed in buffer C as described for CDK1/cyclin B. (Buffer A: 10 mM MgCl2 , 1 mM EGTA, 1 mM dithiothreitol, 25 mM Tris/HCl pH 7.5, 50 μg heparin/mL. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)
Cell Research Cell replication is determined by BrdUrd incorporation after treatment with 1-Azakenpaullone for 24 h. The relative cell number is determined after treatment with 1-Azakenpaullone for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control. (Only for Reference)
Synonyms azakenpaullone
Molecular Weight 328.16
Formula C15H10BrN3O
CAS No. 676596-65-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 61 mg/mL (185.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Kunick C, et al. Bioorg Med Chem Lett. 2004, 14(2), 413-416. 2. Liu H, et al. Diabetes. 2009, 58(3), 663-672. 3. Stukenbrock H, et al. J Med Chem. 2008, 51(7), 2196-2207. 4. Mussmann R, et al. J Biol Chem. 2007, 282(16), 12030-12037. 5. Chan MH, et al. Schizophr Res. 2012, 136(1-3), 96-103.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Kinase Inhibitor Library Anti-Liver Cancer Compound Library Metabolism Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Anti-Ovarian Cancer Compound Library Anti-Cancer Metabolism Compound Library Antioxidant Compound Library Anti-Colorectal Cancer Compound Library

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ABC1183 CHIR-98014 Bakkenolide A GSK3β inhibitor II 5-Iodo-indirubin-3'-monoxime GSK-3β inhibitor 3 GSK-3 Inhibitor 5 ARN25068

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Keywords

1-Azakenpaullone 676596-65-9 PI3K/Akt/mTOR signaling Stem Cells GSK-3 Glycogen synthase kinase-3 1 Azakenpaullone 1Azakenpaullone Glycogen synthase kinase 3 azakenpaullone Inhibitor inhibit 1-Akp inhibitor

 

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