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)
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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