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Bohemine

CAS No. : 189232-42-6

MCE 站：Bohemine

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  MAPK/ERK Pathway

作用靶点：CDK  |  ERK

In Vitro: Bohemine (0-30 ?M; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 ?M 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 ?M) 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 with an IC₅₀ of 27 ?M.

In Vivo: 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.

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