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0.01, 0.10 or 1.00 μM
TAK-243 has weaker inhibitory activity against other closely related E1 ubiquitin-like activating enzymes such as Fat10-activating enzyme (UBA6; 7 ± 3 nM), NEDD8-activating enzyme (NAE; 28 ± 11 nM), SUMO-activating enzyme (SAE; 850 ± 180 nM), ISG15-activating enzyme (UBA7; 5,300 ± 2,100 nM) and autophagy-activating enzyme (ATG7; >10,000 nM) than it does against UAE.
Inhibitory activities of TAK-243 (at 1 μM) against 319 kinases were measured in studies conducted at the Reaction Biology Corporation (Malvem)
