422000

Kenpaullone

A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks).

• Sinónimos: Kenpaullone, 9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704
• Fórmula empírica (notación de Hill): C₁₆H₁₁BrN₂O
• Número de CAS: 142273-20-9
• Peso molecular: 327.18
• Número MDL: MFCD02683595
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow-brown
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C
• InChI: 1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
• Clave InChI: QQUXFYAWXPMDOE-UHFFFAOYSA-N

Descripción

Descripción general

A potent cell-permeable and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC₅₀ = 400 nM), Cdk2/cyclin A (IC₅₀ = 680 nM), Cdk2/cyclin E (IC₅₀ = 7.5 µM), and Cdk5/p25 (IC₅₀ = 850 nM). Also inhibits other kinases such as c-Src (IC₅₀ = 15 µM), casein kinase II (IC₅₀ = 20 µM), ERK1 (IC₅₀ = 20 µM), and ERK2 (IC₅₀ = 9 µM). Inhibition is competitive with respect to ATP binding.

A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC₅₀ = 230 nM), Lck (IC₅₀ = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC₅₀ = 400 nM), Cdk2/cyclin A (IC₅₀ = 680 nM), Cdk2/cyclin E (IC₅₀ = 7.5 µM), and Cdk5/p25 (IC₅₀ = 850 nM). Also inhibits other kinases such as c-Src (IC₅₀ = 15 µM), casein kinase II (IC₅₀ = 20 µM), ERK1 (IC₅₀ = 20 µM), and ERK2 (IC₅₀ = 9 µM). Inhibition is competitive with respect to ATP binding.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Product competes with ATP.

Reversible: yes

Target IC₅₀: 230 nM, 470 nM, 400 nM, 680 nM, 7.5 µM, 850 nM, 15 µM, 20 µM, 20 µM, 9 µM against glycogen synthase kinase-3β, Lck IC50, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, c-Src, casein kinase II, ERK1, and ERK2

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Otras notas

Bain, J., et al. 2003. Biochem. J. 371, 199.
Buolamwini, J.K. 2000. Curr. Pharm. Des.6, 379.
Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3