| Bioactivity | Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 µM), CDK/p35 kinase (IC50=3 µM) and ERK1/p44 MAP kinase (IC50=25 µM)[1][2]. Olomoucine regulates cell cycle and shows anti-melanin tumor activity[3][4]. | ||||||||||||
| Invitro | Olomoucine inhibits CDK2 and CDC2 kinases with IC50 of 7 μM (CDC2/cyclin B), 7 μM (CDK2/cyclin A), 7 μM (CDK2/cyclin E), 3 Μm (CDK5/p35), and 25μM (ERK1/p44 MAPK), respectively[1].Olomoucine (0, 5, 10, 15, and 25 μM) is a competitive inhibitor for ATP and as a non-competitive inhibitor for histone H[1].Olomoucine (0-1000 μM) inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes (CTLL-2 cells) and triggers a Gl arrest similar to interleukin-2 deprivation[2].Olomoucine (0-100 μM) inhibits Gl/S transition of non-small cell lung cancer cell line MB65 cells[2].Olomoucine (0-150 μM) inhibits prophase/metaphase transition of Rdditapes oocytes[2].Olomoucine inhibits tumor cells survival with IC50s of 32.35 μM (dog melanoma), 42.15 μM (mouse B16 melanoma), 82.30 μM (human melanoma), respectively[3]. | ||||||||||||
| In Vivo | Olomoucine (8 mg/kg; i.v.; once daily; 7 d) induces apoptosis in tumor cells on the 3rd day after treatment without side effects[3].Cassette dosing was found to overestimate the AUC while underestimating the Cmax compared with single dosing administration[4].Cassette dosing pharmacokinetics for olomoucine[4] Administration | ||||||||||||
| Name | Olomoucine | ||||||||||||
| CAS | 101622-51-9 | ||||||||||||
| Formula | C15H18N6O | ||||||||||||
| Molar Mass | 298.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Vesely, J., Havlicek, J., Strnad, M., et al. Inhibition of cyclin-dependent kinases by purine analogues. European Journal of Biochemistry 224, 771-786 (1994). [2]. Abraham, R.T., Acquarone, M., Andersen, A., et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biology of the Cell 83(2), 105-120 (1995). [3]. Hajdúch M, et al. Induction of apoptosis and regression of spontaneous dog melanoma following in vivo application of synthetic cyclin-dependent kinase inhibitor olomoucine. Anticancer Drugs. 1997 Nov. 8(10):1007-13. [4]. Raynaud FI, et al. Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. Mol Cancer Ther. 2004 Mar. 3(3):353-62. |
Olomoucine
CAS: 101622-51-9 F: C15H18N6O W: 298.34
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cycli
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