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, 2018, 55(2):1639-1651. 1-Azakenpaullone purchased from Selleck.
Inhibition of GSK3b kinase activity by 1-AKP (100 nmol/L) in the presence or absence of AZD4547. Cells were drug-treated for 48 hours. Immunoblot analysis of total protein extracts following indicated treatments. Dose-response curve shows sensitivity of GAGA6 and GAGA6-R ex vivo-cultured cells to 1-AKP (100 nmol/L) with increasing concentration of AZD4547. Percentage of live cells after drug treatment was determined by Annexin V staining.
Mol Cancer Ther, 2018, 17(1):232-242. 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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Choose Selective GSK-3 Inhibitors
|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.|
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.  In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation.  1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death. 
|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. |
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.)
-  Kunick C, et al. Bioorg Med Chem Lett. 2004, 14(2), 413-416.
-  Liu H, et al. Diabetes. 2009, 58(3), 663-672.
-  Stukenbrock H, et al. J Med Chem. 2008, 51(7), 2196-2207.
|In vitro||DMSO||66 mg/mL (201.12 mM)|
* 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.
C15 H10 Br N3 O
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