E1 activating

PYR-41 is a cell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC50 < 10 μM).

N106, activator of SUMO-activating enzyme, E1 ligase. Increases SERCA2a SUMOylation and activity, and enhances contractility in rat cardiomyocytes in vitro.

2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.

PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay).