JTP 1048196

• CAT Number: I047638
• CAS Number: 55377-56-5
• Molecular Formula: C17H14O4
• Molecular Weight: 282.29
• Purity: ≥95%
• IUPAC Name: 3-[2-(2-methoxyphenyl)-2-oxoethyl]-3H-2-benzofuran-1-one
• InChI: InChI=1S/C17H14O4/c1-20-15-9-5-4-8-13(15)14(18)10-16-11-6-2-3-7-12(11)17(19)21-16/h2-9,16H,10H2,1H3
• SMILES: COC1=CC=CC=C1C(=O)CC2C3=CC=CC=C3C(=O)O2

JTP 1048196 is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 value of 16.1 μM for inhibition of linear polyubiquitination activity by the HOIL-1L/HOIP complex. The lactone structure of JTP 1048196 was transformed to the reactive α,β-unsaturated carbonyl moiety JTP 0819958 (Axon 2939) which reacts with the cysteine residue of LUBAC, leading to its covalent inhibition in vitro and cellular levels.
KEYWORDS: JTP 1048196 | supplier | LUBAC inhibitor | JTP1048196 | JTP-1048196 | CAS [55377-56-5] | NF-κB Pathway | Ubiquitin Ligase (E3; LUBAC) | Inhibitor | Enzymes | HOIL-1L | HOIP | HOIPIN | SHARPIN

Reference

K Katsuya et al. High-Throughput Screening for Linear Ubiquitin Chain Assembly Complex (LUBAC) Selective Inhibitors Using Homogenous Time-Resolved Fluorescence (HTRF)-Based Assay System. SLAS Discov. 2018 Dec;23(10):1018-1029.