货号：P3185

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

Cereblon, encoded by CRBN gene, is the substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins. Cereblon, or the E3 ligase complex mediated normal degradation of key regulatory proteins is required for multiple biological processes, such as normal limb outgrowth. It is well reported that binding of thalidomide-related drugs, such as Lenalidomide, changes the substrate specificity of the E3 ligase complex, leading to decreased degradation of MEIS2 and other target proteins and increased degradation of MYC, IRF4, IKZF1 and IKZF3. Pomalidomide is an analogue of thalidomide. The cellular target of pomalidomide is cereblon. In a fluorescence thermal melt assay utilizing recombinant CRBN (cereblon), it was revealed that pomalidomide bound to cereblon. Pomalidomide increased HbF production in human erythroid cells at the concentration of 1 μM. After incubation for 6 days, pomalidomide induced 2-fold upregulation of γ-globin mRNA levels while decreased β-globin levels 2-fold, also at the concentration of 1 μM. According to another report, pomalidomide was used at the concentrations between 1 nM and 10 μM in both CD4+ and CD8+ cells, pomalidomide significantly elevated IL-2, IL-5, IL-10, and IFN-γ. 8 doses of pomalidomide i.p. administrated at the dose of 0.5 mg/kg among a period of 19 days significantly enhanced the antitumor activity of rituximab in a disseminated lymphoma-bearing SCID mice xenograft model established by i.v. injection of Raji cells. The median survival time of animals treated with pomalidomide and rituximab was 74 days compared to 38 days of those treated with rituximab monotherapy, while pomalidomide was not effective as a single agent.

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