495620

Olomoucine

A purine derivative that acts as a potent, reversible and selective inhibitor of p34^cdk1/cyclin B and related kinases.

• Sinónimos: Olomoucine
• Fórmula empírica (notación de Hill): C₁₅H₁₈N₆O
• Número de CAS: 101622-51-9
• Peso molecular: 298.34
• Número MDL: MFCD00189360
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (TLC)
• Formulario: crystalline solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze
• solubilidad: DMSO: soluble
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C
• cadena SMILES: [n]1(c2nc(nc(c2nc1)NCc3ccccc3)NCCO)C
• InChI: 1S/C15H18N6O/c1-21-10-18-12-13(17-9-11-5-3-2-4-6-11)19-15(16-7-8-22)20-14(12)21/h2-6,10,22H,7-9H2,1H3,(H2,16,17,19,20)
• Clave InChI: GTVPOLSIJWJJNY-UHFFFAOYSA-N

Descripción

Descripción general

A purine derivative that acts as a potent, reversible and selective inhibitor of p34^cdk1/cyclin B (IC₅₀ = 7 µM) and related kinases including p33^cdk2/cyclin A (IC₅₀ = 7 µM), p33^cdk2/cyclin E (IC₅₀ = 7 µM), p33^cdk5/p35 (IC₅₀ = 3 µM), and p44 MAP kinase (IC₅₀ = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34^cdk4/cyclin D (IC₅₀ >1 mM), and p40^cdk6/cyclin D3 (IC₅₀ >250 µM). Does not significantly affect the activity of other protein kinases at 1 mM. Known to inhibit DNA synthesis in interleukin-2-stimulated T lymphocytes and trigger G₁ arrest similar to that observed in interleukin-2-deprived cells. Also used to synchronize cells in G₁. A 50 mM (5 mg/336 µl) solution of Olomoucine (Cat. No. 495624) in DMSOis also available.

A purine derivative that acts as a potent, reversible, and selective inhibitor of p34^cdc2/cyclin B (IC₅₀ = 7 µM) and related kinases, including p33^cdk2/cyclin A (IC₅₀ = 7 µM), p33^cdk2/cyclin E (IC₅₀ = 7 µM), p33^cdk5/p35 (IC₅₀ = 3 µM), and p44^MAPK (IC₅₀ = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34^cdk4/cyclin D1 (IC₅₀ >1000 µM) and p40^cdk6/cyclin D3 (IC₅₀ >250 µM). Does not significantly affect the activity of other protein kinases even at 1 mM concentrations. Known to inhibit DNA synthesis in interleukin-2 stimulated T lymphocytes and triggers G₁ arrest similar to that observed in interleukin-2 deprived cells. Also used to synchronize cells in G₁.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
p34^cdk1/cyclin B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 7 µM, 7 µM, 7 µM, 3 µM, 25 µM against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, and p44 MAP kinase, respectively

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

Abraham, R.T., et al. 1995. Biol. Cell 83, 105.
Mistelli, T., and Warren, G. 1995. J. Cell Sci. 108, 2715.
Glab, N., et al. 1994. FEBS Lett. 353, 207.
Veselý, J., et al. 1994. Eur. J. Biochem.224, 771.

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
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable