| 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;Apoptosis; EpigeneticReaderDomain; AndrogenReceptor |
| 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°C |
| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京