MI-136

MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes. Target: androgen receptorin 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 were bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage. Furthermore, treatment with MI-136 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. [1]in vivo: Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) led to a modest but significant reduction in tumor volume with no effect on mouse body weight. [1]

Signaling Pathways >> Others >> Androgen Receptor

Research Areas >> Cancer

[1]. Malik R, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52.

ARN-509 | Dehydroepiandrosterone | Flutamide | ODM-201 | Danazol | 3,3'-Diindolylmethane | AZD3514 | RAD140 | BMS-564929 | GLPG0492 | Cyproterone acetate | LGD-4033 | Lupeol | Andarine | MK-0773