495620
Olomoucine
A purine derivative that acts as a potent, reversible and selective inhibitor of p34cdk1/cyclin B and related kinases.
Synonym(s):
Olomoucine
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About This Item
Empirical Formula (Hill Notation):
C15H18N6O
CAS Number:
Molecular Weight:
298.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
Assay
≥98% (TLC)
form
crystalline solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
solubility
DMSO: soluble
shipped in
ambient
storage temp.
−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)
InChI key
GTVPOLSIJWJJNY-UHFFFAOYSA-N
General description
A purine derivative that acts as a potent, reversible and selective inhibitor of p34cdk1/cyclin B (IC50 = 7 µM) and related kinases including p33cdk2/cyclin A (IC50 = 7 µM), p33cdk2/cyclin E (IC50 = 7 µM), p33cdk5/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, p34cdk4/cyclin D (IC50 >1 mM), and p40cdk6/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 p34cdc2/cyclin B (IC50 = 7 µM) and related kinases, including p33cdk2/cyclin A (IC50 = 7 µM), p33cdk2/cyclin E (IC50 = 7 µM), p33cdk5/p35 (IC50 = 3 µM), and p44MAPK (IC50 = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34cdk4/cyclin D1 (IC50 >1000 µM) and p40cdk6/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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p34cdk1/cyclin B
p34cdk1/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
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Find documentation for the products that you have recently purchased in the Document Library.
Use of inhibitors in the study of MAPK signaling.
Yoav D Shaul et al.
Methods in molecular biology (Clifton, N.J.), 250, 113-126 (2004-02-03)
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