货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S55781-1ml促销	10mM in DMSO	￥720.00 ￥648.00 S55781-1ml ￥648.00 现货	9 9	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S55781-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

组蛋白甲基转移酶抑制剂;Histone Methyltransferase Inhibitors;;InformationMI-136 MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.TargetsMenin-MLL interactionIn vitroMI-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.In vivoTreatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.Cell Research(from reference)Cell lines：VCaP cells Concentrations：5 μM Incubation Time：48 h

体内研究：

MI-136 在口服给药后 3.1 小时表现出 T1/2。
MI-136 (40 mg/kg，ip) 导致显著减少去势抵抗性 VCaP 肿瘤的生长。

参考文献：

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.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.125 ml	10.627 ml	21.254 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。

参考文献

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