Replaces Prod. #: BML-CC200
Olomoucine is a purine derivative which acts as a potent and selective inhibitor of CDK1 (p34cdc2)/cyclin B and related kinases. It acts by competing for the ATP binding domain of the kinase. Of 35 protein kinases tested, olomoucine inhibited p33CDK2/cyclin A, p33CDK2/cyclin E, p34cdc2/cyclin B, p33CDK5/p35 and erk1 with IC50 of 7, 7, 7, 3 and 25µM respectively. The related kinases p34CDK4/cyclin D and p40CDK6/cyclin D3 were not inhibited or were less sensitive to olomoucine, IC50 > 1000 and 250µM respectively. PKC, PKA, PKG, CaM kinase II, MLC kinase, CK2, EGFR tyrosine kinase, p56lck, p56lyn, p60c-src, v-abl and insulin receptor tyrosine kinase are not inhibited or are weakly inhibited at 1mM. It delays mouse oocyte maturation and inhibits the growth of a variety of human cell lines including Rhabdomyosarcoma cell line Rh1, Rh18, Rh28 and Rh30; MCF-7, KB-3-1 and their adriamycin-resistant counterparts (IC50=18-86µM). It inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes and triggers a G1 arrest similar to interleukin-2 deprivation. Can be used to synchronize cells in G1. Triggers apoptosis in target tumor cells in vitro and in vivo and in maturing cerebellar granule neurons. N9-Isopropyl-olomoucine and the negative control Iso-olomoucine are also available.
Product Details
Alternative Name: | 6-Benzylamino-2-(2-hydroxyethylamino)-9-methylpurine |
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Formula: | C15H18N6O |
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MW: | 298.4 |
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CAS: | 101622-51-9 |
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Purity: | ≥98% |
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Appearance: | White to off-white solid. |
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Solubility: | Soluble in DMSO (32mg/ml), 100% ethanol (7mg/ml), or methanol. |
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Shipping: | Ambient Temperature |
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Long Term Storage: | -20°C |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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67, 1947 (2004),
Abstract;
The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res.
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Abstract;
Chemical inhibitors of cyclin-dependent kinases: L. Meijer, et al.; Meth. Enzymol.
283, 113 (1997),
Abstract;
Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem.
40, 408 (1997),
Abstract;
Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases: R.T. Abraham, et al.; Biol. Cell
83, 105 (1995),
Abstract;
Mitotic disassembly of the Golgi apparatus in vivo: T. Mistelli & G. Warren; J. Cell Sci.
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Abstract;
R.T. Abraham, et al.; Biomed. J. 1, 32 (1994),
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesely, et al.; Eur. J. Biochem.
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Abstract;