The chemical structure of SDX-7320 is shown in Fig. 1, along with the pharmacologically active small molecule METAP2 inhibitor SDX-7539. The preparation and characterization of SDX-7320 and SDX-7539 are described in the Supplementary Data and in Supplementary Fig. S1 and Supplementary Table S1, along with the related compounds SDX-9246, SDX-9280, SDX-9178, TNP-470, and CKD-732. The benzenesulfonic acid salt form of SDX-7539 (SDX-9402) was used for in vitro experiments.