Probe Selectivity in Vitro:
TAK-243 has significant biochemical inhibitory activity against closely related E1 ubiquitin-like activating enzymes Fat10-activating enzyme (UBA6; 7 ± 3 nM) and NEDD8-activating enzyme (NAE; 28 ± 11 nM) but has better biochemical selectivity for UBA1 over SUMO-activating enzyme (SAE; 850 ± 180 nM), ISG15-activating enzyme (UBA7; 5,300 ± 2,100 nM), and autophagy-activating enzyme (ATG7; >10,000 nM).
Outside target family: Tested on Novascreen Receptor Panel (at 1 µM TAK-243; minimal findings) and carbonic anhydrases. Inhibitory activities of 1 µM TAK-243 against 319 kinases were measured at Reaction Biology Corporation (Malvern, PA) with no significant findings.
