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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MI-136
CAS number：1628316-74-4 molecular formula：C23H21F3N6S
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| Chinese alias | - | ||
| English alias | 1H-Indole-2-carbonitrile,5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]- | ||
| CAS number | 1628316-74-4 | molecular formula | C23H21F3N6S |
| molecular weight | 470.51 g/mol | Exact mass | 10mM in DMSO |
| PSA | 109.000 Ų | logp | 4.886 |
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