HOIPIN 11a

• CAT Number: I047643
• CAS Number: 1610800-91-3
• Molecular Formula: C15H18N2O4
• Molecular Weight: 290.31
• Purity: ≥95%
• IUPAC Name: methyl (E)-4-[(2-oxo-5,6,7,8-tetrahydro-1H-quinoline-3-carbonyl)amino]but-2-enoate
• InChI: InChI=1S/C15H18N2O4/c1-21-13(18)7-4-8-16-14(19)11-9-10-5-2-3-6-12(10)17-15(11)20/h4,7,9H,2-3,5-6,8H2,1H3,(H,16,19)(H,17,20)/b7-4+
• SMILES: COC(=O)/C=C/CNC(=O)C1=CC2=C(CCCC2)NC1=O

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

Reference

H Johansson et al. Fragment-Based Covalent Ligand Screening Enables Rapid Discovery of Inhibitors for the RBR E3 Ubiquitin Ligase HOIP. J Am Chem Soc. 2019 Feb 13;141(6):2703-2712.