中文名：MI-136
英文名：MI-136
纯度：≥98%
货号：M413840
Cas号：1628316-74-4
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
MI-136 MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.
Targets
Menin-MLL interaction
In vitro
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.
In vivo
Treatment 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
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关键字： 1H-?Indole-?2-?carbonitrile,5-?[[4-?[[6-?(2,?2,?2-?trifluoroethyl)?thieno[2,?3-?d]?pyrimidin-?4-?yl]?amino]?-?1-?piperidinyl]?methyl]?-
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