495620

Olomoucine

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

• Sinonimo/i: Olomoucine
• Formula empirica (notazione di Hill): C₁₅H₁₈N₆O
• Numero CAS: 101622-51-9
• Peso molecolare: 298.34
• Numero MDL: MFCD00189360
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (TLC)
• Forma fisica: crystalline solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Solubilità: DMSO: soluble
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°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); GTVPOLSIJWJJNY-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable