uba1

TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis.

NSC624206 is a ubiquitin E1 (UBA1) inhibitor(IC50 of ~9 μM).

PYZD-4409 is a selective UBA1 inhibitor with an IC50 of 20 μM. PYZD-4409 induces cell death in malignant cells and is preferentially cytotoxic to malignant cells over normal hematopoietic cells.

Ubiquitination-IN-2 is a potent inhibitor of E1-E2 protein−protein interactions (PPI), exhibiting inhibitory activity with a dissociation constant (Kd) of 0.72 μM for the ubiquitin E1 (Uba1) enzyme. By blocking the transfer of ubiquitin from E1 to E2, Ubiquitination-IN-2 serves as a valuable tool in cancer research [1].