1-Azakenpaullone

Names

[ Name ]:
1-Azakenpaullone

[Synonym ]:
Pyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one, 9-bromo-7,12-dihydro-
azakenpaullone
9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one
9-Bromo-7,12-dihydro-pyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one
1-Azakenpaullone
Kinome_3492
HMS3229B07

Biological Activity

[Description]:

1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Research Areas >> Metabolic Disease

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

GSK-3β:18 nM (IC50)

CDK1/cyclin B:2 μM (IC50)

CDK5/p25:4.2 μM (IC50)

[References]

[1]. Kunick C, et al. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
648.8±50.0 °C at 760 mmHg

[ Melting Point ]:
>290ºC (dec.)

[ Molecular Formula ]:
C₁₅H₁₀BrN₃O

[ Molecular Weight ]:
328.163

[ Flash Point ]:
346.2±30.1 °C

[ Exact Mass ]:
327.000702

[ PSA ]:
57.78000

[ LogP ]:
3.19

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.740

[ Storage condition ]:
-20°C Freezer

[ Water Solubility ]:
DMSO: >10mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Efficient definitive endoderm induction from mouse embryonic stem cell adherent cultures: a rapid screening model for differentiation studies.

Stem Cell Res. 12(1) , 166-77, (2014)

Definitive endoderm (DE) differentiation from mouse embryonic stem cell (mESC) monolayer cultures has been limited by poor cell survival or low efficiency. Recently, a combination of TGFβ and Wnt acti...

WNT3 and membrane-associated β-catenin regulate trophectoderm lineage differentiation in human blastocysts.

Mol. Hum. Reprod. 21 , 711-22, (2015)

WNT/β-catenin signaling has been described as a crucial regulator of embryonic stem cells and embryogenesis. However, little is known on its role during human preimplantation embryo development, besid...

GSK3β-dependent phosphorylation alters DNA binding, transactivity and half-life of the transcription factor USF2.

PLoS ONE 9(9) , e107914, (2014)

The upstream stimulatory factor 2 (USF2) is a regulator of important cellular processes and is supposed to have also a role during tumor development. However, the knowledge about the mechanisms that c...

Related Compounds

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