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Bohemine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bohemine图片
CAS NO:189232-42-6
包装与价格:
包装价格(元)
5mg询价
25mg询价

Bohemine 是一种嘌呤类似物,是一种合成的选择性 CDK 抑制剂,对 Cdk2/cyclin E、Cdk2/cyclin A 和 Cdk9/cyclin T1 的 IC50 分别为 4.6 μM、83 μM 和 2.7 μM。 Bohemine 还抑制 ERK2,IC50 为 52 μM,对 CDK1、CDK4 和 CDK6 的抑制作用较小。 Bohemine具有广谱抗癌活性。
Cas No.189232-42-6
化学名3-((6-(benzylamino)-9-isopropyl-9H-purin-2-yl)amino)propan-1-ol
Canonical SMILESCC(N1C=NC(C1=NC(NCCCO)=N2)=C2NCC3=CC=CC=C3)C
分子式C18H24N6O
分子量340.42
溶解度≥ 17mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 1 μM for cyclin-dependent kinase

A highly conserved array of mechanisms regulating cyclin-dependent kinases (CDK), which govern the timing of cell cycle progression and division, has developed in eukaryotes. CDK inhibitors have been shown to play an key regulatory role in cell proliferation, differentiation, senescence, as well as programmed death.

In vitro: Bohemine was applied to cultures of mouse hybridoma cells in order to evaluate its capacity of cell growth and the production of monoclonal antibody. Results showed that addition of bohemine at concentrations in the range of 1-10 μM led to a short-term arrest of growth and monoclonal antibody production. Such short-term suppression of cell functions was followed by a significant temporary increase of specific growth rate and specific production rate. In semicontinuous cultures, the steady-state viable cell density values showed a certain stimulation of cell growth in the presence of bohemine at micromolar concentrations, and growth inhibition at 10 and 30 μM [1].

In vivo: In mice, bohemine was found to be rapidly and completely metabolized and disappeared from circulation during the first 60 min following i.v. administration. Moreover, the metabolites were eliminated by the hepatobiliary tract and also by renal excretion [2].

Clinical trial: Up to now, bohemine is still in the preclinical development stage.

References:
[1] Franek F,Strnad M,Havlícek L,Siglerová V,Fismolová I,Eckschlager T.  Diverse effects of the cyclin-dependent kinase inhibitor bohemine: Concentration- and time-dependent suppression or stimulation of hybridoma culture. Cytotechnology.2001 Jul;36(1-3):117-23.
[2] Chmela Z,Vesel J,Lemr K,Rypka M,Hanus J,Havlícek L,Krystof V,Michnová L,Fuksová K,Lukes J.  In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route. Drug Metab Dispos.2001 Mar;29(3):326-34.

 
 
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