S81382 |
MI-136 |
| 源叶(MedMol) | ≥98% |
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- 产品描述： MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced
- 靶点： Androgen Receptor;Apoptosis;Epigenetic Reader Domain
- 体外研究： MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer.
- 体内研究： Treatment of VCaP tumor-bearing mice with MI-136 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.
- 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)
- 参考文献：
1. Malik R, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015, 21(4):344-352.
- 溶解性： Soluble in DMSO、Ethanol
- 保存条件： -20℃
- 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 50 mM 0.043 ml 0.213 ml 0.425 ml
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