AR阳性细胞系如VCaP, LNCaP and 22RV1对MI-136具有敏感性,进行MI-136的处理会抑制在AR刺激后与ASH2L结合的基因的表达、诱导VCaP细胞的凋亡,在AR依赖性细胞系(LNCaP和VCaP)中阻止DHT诱导的细胞增殖。MI-136对细胞增殖的作用类似于MDV-310(第二代FDA认证的抗雄激素药物,用于治疗难治性前列腺癌)
1. Dmitry Borkin, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.2. Rohit Malik, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52.
MI-136 - 配置溶液浓度参考
1mg
5mg
10mg
1 mM
2.125 ml
10.627 ml
21.253 ml
5 mM
0.425 ml
2.125 ml
4.251 ml
10 mM
0.213 ml
1.063 ml
2.125 ml
5 mM
0.043 ml
0.213 ml
0.425 ml
最后更新:2024-01-02 23:10:35
MI-136 - 细胞实验
To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference) Cell lines: VCaP cells