495620

Olomoucine

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

• 同義詞: Olomoucine
• 經驗公式（希爾表示法）: C₁₅H₁₈N₆O
• CAS號碼: 101622-51-9
• 分子量：: 298.34
• MDL號碼: MFCD00189360
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (TLC)
• 形狀: crystalline solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze
• 溶解度: DMSO: soluble
• 運輸包裝: ambient
• 儲存溫度: −20°C
• SMILES 字串: [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)
• InChI 密鑰: GTVPOLSIJWJJNY-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

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

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable