1-Azakenpaullone

Catalog No.S7193 Batch:S719301

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Technical Data

Formula

C15 H10 Br N3 O

Molecular Weight 328.16 CAS No. 676596-65-9
Solubility (25°C)* In vitro DMSO 66 mg/mL (201.12 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.3mg/ml Taking the 1 mL working solution as an example, add 50 μL 66 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 induced locomotor hyperactivity, disruption of PPI and cognitive deficits, and improves the 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. Buffer C: homogenization buffer but 5 mM EGTA, no NaF and no protease inhibitors.)

Cell Assay:

[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.

Animal Study:

[5]

  • Animal Models

    Male NMRI mice

  • Dosages

    ~500 pmol

  • Administration

    i.c.v.

Customer Product Validation

, , Mol Neurobiol, 2018, 55(2):1639-1651

, , Dev Genes Evol, 2015, 225(1):47-53.

Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(1):232-242]

Selleck's 1-Azakenpaullone has been cited by 16 publications

Cellular remodeling and JAK inhibition promote zygotic gene expression in the Ciona germline [ EMBO Rep, 2024, 25(5):2188-2201] PubMed: 38649664
Patterns of NFkB activation resulting from damage, reactive microglia, cytokines, and growth factors in the mouse retina [ Exp Neurol, 2023, 359:114233] PubMed: 36174748
Induction of mouse totipotent stem cells by a defined chemical cocktail [ Nature, 2022, 10.1038/s41586-022-04967-9] PubMed: 35728625
Filamin C regulates skeletal muscle atrophy by stabilizing dishevelled-2 to inhibit autophagy and mitophagy [ Mol Ther Nucleic Acids, 2022, 27:147-164] PubMed: 34976434
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Overexpression of ubiquitin-conjugating enzyme E2 L3 in hepatocellular carcinoma potentiates apoptosis evasion by inhibiting the GSK3β/p65 pathway. [ Cancer Lett, 2020, 1;481:1-14] PubMed: 32268166
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
BYSL Promotes Glioblastoma Cell Migration, Invasion, and Mesenchymal Transition Through the GSK-3β/β-Catenin Signaling Pathway [ Front Oncol, 2020, 10:565225] PubMed: 33178594
Targeting Degradation of the Transcription Factor C/EBPβ Reduces Lung Fibrosis by Restoring Activity of the Ubiquitin-Editing Enzyme A20 in Macrophages [ Immunity, 2019, 51(3-:522-534] PubMed: 31471107
Mapping phospho-catalytic dependencies of therapy-resistant tumours reveals actionable vulnerabilities. [ Nat Cell Biol, 2019, 21(6):778-790] PubMed: 31160710

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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