Bohemine

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Bohemine  纯度: ≥98.0%

Bohemine 是一种嘌呤类似物，也是一种合成的选择性的 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 具有广泛的抗癌活性。

Bohemine

Bohemine Chemical Structure

CAS No. : 189232-42-6

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生物活性

Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities[1][2].

IC50 & Target[2]

CDK2/cyclinE

4.6 μM (IC50)

cdk2/cyclin A

83 μM (IC50)

CDK9/cyclinT1

2.7 μM (IC50)

ERK2

52 μM (IC50)

体外研究
(In Vitro)

Bohemine (0-30 µM; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 µM results in a short-term arrest of growth and of monoclonal antibody production. The short-term suppression of cell functions is followed by a significant temporary increase of specific growth rate and of specific production rate[1].
Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 µM) concentration[1].
T-lymphoblastic cell line CEM is treated by Bohemine, five proteins are found to be downregulated, namely α-enolase, triosephosphate isomerase, initiation factor 5A, and α- and β-subunits of Rho GDP-dissociation inhibitor 1. These proteins play significant roles in glycolysis, proteosynthesis, and in cytoskeleton rearrangement[1].
Bohemine inhibits growth of human tumor cell lines with an IC50 of 27 µM[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Mouse hybridoma ME-750 cells
Concentration: 0 µM, 1 µM, 3 µM, 10 µM and 30 µM
Incubation Time: 72 hours
Result: At 10 µM and 30 µM concentrations, the viable cell count was significantly lower with respect to control, i.e., 77% and 48%, respectively.

体内研究
(In Vivo)

Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice bearing the colon 26 murine tumor[2]
Dosage: 50 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
Result: Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h.

分子量

340.42

Formula

C18H24N6O
CAS 号

189232-42-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Franek F, et al. 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]. Raynaud FI, et al. In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clin Cancer Res. 2005 Jul 1;11(13):4875-87.

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