1-Azakenpaullone

Name: 1-Azakenpaullone
Brand: Tocris Bioscience
SKU: 3673

Tocris Bioscience, part of Bio-Techne | Catalog # 3673

COA / SDS

Potent and selective GSK3 inhibitor. Used in chemical cocktail for induction and maintainance of TotiSCs.

Key Product Details

Description:	Potent and selective GSK3 inhibitor. Used in chemical cocktail for induction and maintainance of TotiSCs.
Alternative Names:	1-Akp
Chemical Name:	9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one
Purity:	≥98% (HPLC)
Molecular Weight:	328.17

View Full Technical Details for 1-Azakenpaullone

Technical Data
Citations

Biological Activity for 1-Azakenpaullone

1-Azakenpaullone is a potent and selective inhibitor of glycogen synthase kinase 3 (GSK-3), with IC₅₀ = 18 nM. It displays selectivity index (SI) of 111 and 233 over CDK1 and CDK5, respectively.

1-Azakenpaullone stimulates growth and replication of β-cells in vitro (rat islets) and alleviates glucolipotoxicity in INS-1 β-cells. It displays mitogenic effects on rat β-cells comparable with those of incretin hormone GIP.

In combination with TTNPB (Cat. No. 0761) and WS 6 (Cat. No. 7791), 1-Azakenpaullone can be part of a chemical cocktail used for induction and long-term maintainance in vitro of totipotent stem cells (TotiSCs) from mouse pluripotent stem cells (PSCs).

Technical Data for 1-Azakenpaullone

M. Wt	328.17
Formula	C₁₅H₁₀BrN₃O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	676596-65-9
PubChem ID	6538897
InChi Key	NTSBZVCEIVPKBJ-UHFFFAOYSA-N
Smiles	BrC2=CC=C1NC3=C(CC(NC4=C3N=CC=C4)=O)C1=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for 1-Azakenpaullone

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	32.82	100

Preparing Stock Solutions for 1-Azakenpaullone

The following data is based on the product molecular weight 328.17.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.05 mL	15.24 mL	30.47 mL
5 mM	0.61 mL	3.05 mL	6.09 mL
10 mM	0.30 mL	1.52 mL	3.05 mL
50 mM	0.06 mL	0.30 mL	0.61 mL

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References for 1-Azakenpaullone

References are publications that support the biological activity of the product.

Mussmann Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. J.Biol.Chem. 2007 PMID: 17242403
Hu Induction of mouse totipotent stem cells by a defined chemical cocktail. Nature 2023 PMID: 35728625
Kunick 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β. Bioorg.Med.Chem.Lett. 2004 PMID: 14698171