1-Azakenpaullone

Catalog No.S7193

1-Azakenpaullone Chemical Structure

Molecular Weight(MW): 328.16

1-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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  • Wnt activation stimulates proliferation in irradiated neuromasts. Radiated larvae were treated with 2.5 μM Az at 48 h after IR for 2 days. Representative images of YO-PRO1 staining for HCs in radiated neuromasts in larvae treated with DMSO (a) and Az (b). c Two days after 30 Gy IR, larvae treated with 2.5 μM Az for 2 days. Two-tailed t test analysis of the number of HCs in neuromasts revealed a significant increase in Az-treated larvae compared to those treated with DMSO during the two incubation days (eight fish per group; N = 3, two-tailed t test, **p < 0.01, ***p < 0.001). d-e Representative images of BrdU staining for proliferation in radiated neuromasts in larvae treated with DMSO (d) and Az (e). Neuromasts were counterstained by SYTOX. f Two-tailed t test analysis of the number of BrdU+ cells in neuromasts revealed a significantly increase in Az-treated larvae compared to those treated with DMSO during the three incubation days (n = 8 fish per group; N = 3, two-tailed t test, *p < 0.05, **p < 0.01, ***p < 0.001). Scale bar 10 μm

    Mol Neurobiol, 2017. 1-Azakenpaullone purchased from Selleck.

    Expression of negaly6 was normally expressed in the trailing zone of pLLp in 1-azakenpaullone (i, i′)- or XAV-939 (j, j′)-treated embryos. Compared with the expression of dkk1 in DMSO-treated embryos(e, e′), its expression was increased in 1-azakenpaullonetreated embryos (f, f′) and reduced in XAV-939-treated embryos (g, g′). Cell nucleus were stained with SYTOX® green nucleic acid stain(green). The pLLp was enclosed by white dotted line.

    Dev Genes Evol, 2015, 225(1):47-53.. 1-Azakenpaullone purchased from Selleck.

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Biological Activity

Description 1-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
GSK-3α [1] GSK-3β [1]
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

Kinase Assay:

[6]

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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]

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  • 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]

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  • Animal Models: Male NMRI mice
  • Formulation: 1% DMSO in artificial cerebrospinal fluid (ACSF)
  • 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 powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID