Olomoucine (high purity)

CDK/cyclin inhibitor



ALX-350-013-M005	5 mg	100.00 USD

ALX-350-013-M025	25 mg	371.00 USD
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Replaces Prod. #: BML-CC200

Olomoucine is a purine derivative which acts as a potent and selective inhibitor of CDK1 (p34^cdc2)/cyclin B and related kinases. It acts by competing for the ATP binding domain of the kinase. Of 35 protein kinases tested, olomoucine inhibited p33^CDK2/cyclin A, p33^CDK2/cyclin E, p34^cdc2/cyclin B, p33^CDK5/p35 and erk1 with IC₅₀ of 7, 7, 7, 3 and 25µM respectively. The related kinases p34^CDK4/cyclin D and p40^CDK6/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, p56^lck, p56^lyn, p60^c-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

Formula:	C₁₅H₁₈N₆O

MW:	298.4

CAS:	101622-51-9

Purity:	≥98%

Appearance:	White to off-white solid.

Solubility:	Soluble in DMSO (32mg/ml), 100% ethanol (7mg/ml), or methanol.

Shipping:	Ambient Temperature

Long Term Storage:	-20°C

Regulatory Status:	RUO - Research Use Only

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Product Literature References

Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 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. 245, 8 (1998), 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. 108, 2715 (1995), 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. 224, 771 (1994), Abstract;