MI-136 (C09-0967-570)

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. Specifications and Purity: ≥98%. Molecular Formula: C23H21F3N6S. Molecular Weight: 470.51. PubChem CID: 86297077. Isomeric SMILES: C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N.