MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM). By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription. At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.
