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 is a purine analogue and is a synthetic and selective CDK inhibitor with IC 50 s 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 IC 50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.

Solid

CDK2/cyclinE 4.6 μM (IC50) cdk2/cyclin A 8

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.
Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 μM) concentration.
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.
Bohemine inhibits growth of human tumor cell lines

Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows C max is 72,308 nM, observed clearance is 0.23 L/h and T 1/2 is 1.39 h. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[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.

In Vitro: DMSO : 100 mg/mL (293.75 mM; Need ultrasonic)配制储备液