Inspiredby the unique properties of engagement between complex 9 and SET7, we combined the two rigid 1-phenylisoquinoline C∧N ligands of complex 9 with a 5,6-dimethyl-1,10-phenanthrolineN∧N ligand from a bioavailable selective inhibitorof the MLL–menin PPI to obtaina dual targeting rhodium­(III) scaffold, complex 10 (Figure E). The hybrid complex 10 bound to the SAM bindingpocket of SET7 and disrupted the menin–MLL PPI, eventuallyinhibiting the activity of the androgen receptor for treating castration-resistantprostate cancer. Here, KMT2A is linked to cancer.