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Merck

191500

1-Azakenpaullone

A Kenpaullone analog that acts as a potent and ATP-competitive inhibitor of GSK-3β.

Synonym(s):

1-Azakenpaullone, 1-AKP

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About This Item

Empirical Formula (Hill Notation):
C15H10BrN3O
CAS Number:
676596-65-9
Molecular Weight:
328.16
UNSPSC Code:
12352200
MDL number:
MFCD09037522

Key Documents

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Product Name

1-Azakenpaullone, A Kenpaullone analog that acts as a potent and ATP-competitive inhibitor of GSK-3β.

InChI

1S/C15H10BrN3O/c16-8-3-4-11-9(6-8)10-7-13(20)18-12-2-1-5-17-15(12)14(10)19-11/h1-6,19H,7H2,(H,18,20)

InChI key

NTSBZVCEIVPKBJ-UHFFFAOYSA-N

assay

≥94% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

tan

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Biochem/physiol Actions

Cell permeable: no
Primary Target
GSK-3β
Product competes with ATP.
Reversible: no
Target IC50: 18 nM against GSK-3β

Disclaimer

Toxicity: Standard Handling (A)

General description

A Kenpaullone (Cat. No. 422000) analog that acts as a potent and ATP-competitive inhibitor of GSK-3β (IC50 = 18 nM). Displays over 100-fold greater selectivity over Cdk1/cyclin B and Cdk5/p25 (IC50 = 2.0 µM and 4.2 µM, respectively).
A Kenpaullone (Cat. No. 422000 ) analog that acts as a potent and ATP-competitive inhibitor of GSK-3β (IC50 = 18 nM), and displays ~100-200 fold greater selectivity over Cdk1/B and Cdk5/p25 (IC50 = 2 µM and 4.2 µM, respectively). Also available as a 10 mM solution in DMSO (Cat. No. 191501).

Other Notes

Kunick, C., et al. 2004. Bioorg. Med. Chem. Lett.14, 413.

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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