1-Azakenpaullone

Catalog No.S7193 Synonyms: 1-Akp

For research use only.

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

1-Azakenpaullone Chemical Structure

CAS No. 676596-65-9

Selleck's 1-Azakenpaullone has been cited by 11 Publications

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Biological Activity

Description 1-Azakenpaullone (1-Akp) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.
Targets
GSK-3α [1] GSK-3β [1]
(Cell-free assay)
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 deficits, and improves the ketamine-induced motor incoordination in rotarod test. [5]

Protocol (from reference)

Kinase Assay:

[6]

  • 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:

[4]

  • Cell lines: INS-1E β cell
  • Concentrations: 20 μM
  • Incubation Time: 4 days
  • Method:

    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)
Animal Research:

[5]

  • Animal Models: Male NMRI mice
  • Dosages: ~500 pmol
  • Administration: i.c.v.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 66 mg/mL
(201.12 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 328.16
Formula

C15 H10 Br N3 O

CAS No. 676596-65-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br

In vivo Formulation Calculator (Clear solution)

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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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