191500

1-Azakenpaullone

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

• Synonym(s): 1-Azakenpaullone, 1-AKP
• Empirical Formula (Hill Notation): C₁₅H₁₀BrN₃O
• CAS Number: 676596-65-9
• Molecular Weight: 328.16
• MDL number: MFCD09037522
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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
• 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

Description

General description

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).

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).

Biochem/physiol Actions

Cell permeable: no

Primary Target
GSK-3β

Product competes with ATP.

Reversible: no

Target IC₅₀: 18 nM against GSK-3β

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable