126870

Alsterpaullone

A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3β (IC₅₀ = 4 nM) and Cdk1/cyclin B (IC₅₀ = 35 nM).

• Synonim(y): Alsterpaullone, 9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, 9-Nitropaullone, NSC 705701
• Wzór empiryczny (zapis Hilla): C₁₆H₁₁N₃O₃
• Numer CAS: 237430-03-4
• Masa cząsteczkowa: 293.28
• Numer MDL: MFCD02683579
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: light yellow to brown
• rozpuszczalność: DMSO: 20 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• InChI: 1S/C16H11N3O3/c20-15-8-12-11-7-9(19(21)22)5-6-14(11)18-16(12)10-3-1-2-4-13(10)17-15/h1-7,18H,8H2,(H,17,20)
• Klucz InChI: OLUKILHGKRVDCT-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
GSK-3β, Cdk1/cyclin B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 4 nM, 35 nM, against GSK-3β, Cdk1/cyclin B, respectively

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3