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Olomoucine

(Synonyms: 2-(2'-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤) 目录号 : GC16520

An inhibitor of cyclin-dependent kinases

Olomoucine Chemical Structure

Cas No.:101622-51-9

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1mg
¥444.00
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5mg
¥967.00
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10mg
¥1,713.00
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25mg
¥3,760.00
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产品描述

Olomoucine is an ATP-competitive CDK inhibitor [1].

Cyclin-dependent kinases (CDKs) play important roles in the regulation of the cell division cycle and are therefore promising targets for cancer therapy [1].

Olomoucine is an ATP-competitive CDK inhibitor with IC50 values of 7, 7, 7, 3 and 25 μM against CDC2/cyclin B, Cdk2/cyclin A and Cdk2/cyclin E kinases, the brain CDK5/p35 kinase and the ERK1/p44 MAP kinase, respectively [1]. In metaphase-arrested Xenopus egg extracts, Olomoucine inhibited M-phase-promoting factor activity. Olomoucine provided an anti-mitotic reagent that might preferentially inhibit certain steps of the cell cycle [1]. In interleukin-2-stimulated T lymphocytes (CTLL-2 cells), Olomoucine inhibited DNA synthesis and caused Gl arrest [2].

In rats after after spinal cord injury (SCI), olomoucine attenuated astroglial proliferation and glial scar formation, decreased lesion cavity and mitigated functional deficits. In rats following SCI, olomoucine significantly decreased the spinal cord edema formation, suppressed microglial proliferation and attenuated production of proinflammatory cytokines in the traumatic spinal cord. Olomoucine also attenuated neuronal cell death [3].

References:
[1].  Vesel J, Havlicek L, Strnad M, et al. Inhibition of cyclin-dependent kinases by purine analogues. Eur J Biochem. 1994 Sep 1;224(2):771-86.
[2].  Abraham RT, Acquarone M, Andersen A, et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biol Cell. 1995;83(2-3):105-20.
[3].  Tian DS, Xie MJ, Yu ZY, et al. Cell cycle inhibition attenuates microglia induced inflammatory response and alleviates neuronal cell death after spinal cord injury in rats. Brain Res. 2007 Mar 2;1135(1):177-85.

Chemical Properties

Cas No. 101622-51-9 SDF
别名 2-(2'-羟基乙基氨基)-9-甲基-6-(苄基氨基)嘌呤
化学名 2-[[9-methyl-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-ethanol
Canonical SMILES OCCNc1nc(NCc2ccccc2)c2ncn(C)c2n1
分子式 C15H18N6O 分子量 298.3
溶解度 ≤10mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mM 3.3523 mL 16.7616 mL 33.5233 mL
5 mM 0.6705 mL 3.3523 mL 6.7047 mL
10 mM 0.3352 mL 1.6762 mL 3.3523 mL
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