Alsterpaullone-CAS 237430-03-4-Calbiochem

C₁₆H₁₁N₃O₃

293.28

MFCD02683579

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM). Displays remarkable in vitro antitumor activity. Inhibits Tau phosphorylation at sites that are typically phosphorylated by GSK-3β in Alzheimer’s disease. Also inhibits Cdk5/p25-dependent phosphorylation of DARPP-32.
A cell-permeable, potent, reversible, and ATP competitive inhibitor of cdk1/cyclin B (IC₅₀ = 35 nM) and GSK-3β (IC₅₀ = 4 nM). One of the most active paullones that acts by competing with ATP for binding to GSK-3β and inhibits the phosphorylation of tau. Also inhibits the activity of Cdk5/p25-dependent phosphorylation of DARPP-32 (a 32 kDa dopamine and adenosine 3′,5′-monophosphate-regulated phosphoprotein). Displays remarkable antitumor activity in vitro. Inhibits growth of the colon cancer cell line HCT-116, with an IC₅₀ in the nanomolar range.

Cell permeable: yes
Target IC₅₀: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively
Product competes with ATP.
Reversible: yes
Primary Target
GSK-3β, Cdk1/cyclin B

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Leost, M., et al. 2000. Eur. J. Biochem.267, 5983.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

light yellow to brown

DMSO: 20 mg/mL

ambient

−20℃

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3