1-Azakenpaullone A Kenpaullone analog and an inhibitor of GSK-3

1-Azakenpaullone (CAS 676596-65-9)

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Synonym: 9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one; 1-AKP; kenpaullone;
Application: A Kenpaullone analog and an inhibitor of GSK-3
CAS Number: 676596-65-9
Molecular Weight: 328.20
Molecular Formula: C15H10BrN3O
* Refer to Certificate of Analysis for lot specific data (including water content).
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1-Azakenpaullone is a Kenpaullone analog shown to act as a potent and ATP-competitive inhibitor of GSK-3β, and displays ~100-200 fold greater selectivity over Cdk1/B and Cdk5/p25.


References

1. Kunick, Conrad., et al., 2004. 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorganic & medicinal chemistry letters. 14(2): 413-6. PMID: 14698171

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/ml), and methanol. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
>250° C (dec.)
Boiling Point :
648.83° C at 760 mmHg (Predicted)
Density :
1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.74 (Predicted)
IC50 :
GSK-3β: IC50 = 18 nM; Cdk1/cyclin B: IC50 = 2.0 µM; Cdk5/p25: IC50 = 4.2 µM
Ki Data :
GSK-3α: Ki= 5.01 nM (human); GSK-3β: Ki= 10 nM (human); Fyn: Ki= 100 nM (human); Flt-1: Ki>398.11 nM (human); Cdk2: Ki= 501.19 nM (human)
pK Values :
pKa: 13.36 (Predicted), pKb: 3.82 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
PubChem CID :
6538897
MDL Number :
MFCD09037522
SMILES :
C1C2=C(C3=C(C=CC=N3)NC1=O)NC4=C2C=C(C=C4)Br

Download SDS (MSDS)

Certificate of Analysis

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