Selective, cell-permeable and covalent inhibitor of the RBR E3 ubiquitin ligase HOIP. Biochemical characterization of HOIPIN 11a demonstrated that this compound labels HOIP with promising proteome-wide selectivity and effectively inhibits linear polyubiquitin chain formation in vitro and in a cellular environment. Treating HEK293T cells overexpressing full length HOIP, HOIL-1L, and SHARPIN with compound 11a overnight led to inhibition of NF-κB activation in a concentration-dependent manner, with an estimated IC50 value of 37 μM.

KEYWORDS: HOIPIN 11a | supplier | HOIP inhibitor | GSK11a | GSK 11a | GSK-11a | CAS [1610800-91-3] | NF-κB Pathway | Ubiquitin Ligase (E3; LUBAC) | Inhibitor | Enzymes | HOIL-1L | SHARPIN | E3 ligase