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.
2 Customer Reviews
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.
Purity & Quality Control
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
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.