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

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1-Azakenpaullone GSK-3 inhibitor

Cat.No.S7193

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

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 328.16 Formula

C15 H10 Br N3 O

 Storage (From the date of receipt)
CAS No. 676596-65-9 -- Storage of Stock Solutions

Synonyms 1-Akp Smiles C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (201.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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, 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.)
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17242403/
  • [5] https://pubmed.ncbi.nlm.nih.gov/22325078/
  • [6] https://pubmed.ncbi.nlm.nih.gov/10998059/

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