Home PI3K/Akt/mTOR GSK-3 inhibitor 1-Azakenpaullone

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1-Azakenpaullone GSK-3 inhibitor

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 GSK-3 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 328.16

Purity & Quality Control

Batch: S719301 DMSO]66 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.66%
99.66

Related Products

Signaling Pathway

GSK-3 Signaling Pathways

GSK-3 Signaling Pathway

Mechanism of Action

Targets
GSK-3α [1] GSK-3β [1]
(Cell-free assay)
18 nM

In vitro
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, this compound (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. [2] It effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. [3][4]
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. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)
Cell Research 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 this compound for 4 days using the CyQuant cell proliferation assay. Results are presented as fold change relative to control.

In Vivo
In vivo

Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the induced locomotor hyperactivity, disruption of PPI and cognitive deficits, and improves the induced motor incoordination in rotarod test. [5]
Animal Research Animal Models Male NMRI mice
Dosages ~500 pmol
Administration i.c.v.

References
  • https://pubmed.ncbi.nlm.nih.gov/14698171/
  • https://pubmed.ncbi.nlm.nih.gov/19073772/
  • https://pubmed.ncbi.nlm.nih.gov/18345612/
  • https://pubmed.ncbi.nlm.nih.gov/17242403/
  • https://pubmed.ncbi.nlm.nih.gov/22325078/
  • https://pubmed.ncbi.nlm.nih.gov/10998059/

Chemical Information

Molecular Weight 328.16 Formula

C15 H10 Br N3 O
CAS No. 676596-65-9 SDF --
Synonyms 1-Akp
Smiles C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (201.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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