1414882-10-2

Basic information

• Product Name: 8,8’-disulfanediylbis(N-benzylquinoline-3-carboxamide)
• Synonyms: 8,8’-disulfanediylbis(N-benzylquinoline-3-carboxamide)
• CAS NO: 1414882-10-2
• Molecular Weight: 586.738
• Mol File: 1414882-10-2.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: 8,8’-disulfanediylbis(N-benzylquinoline-3-carboxamide)(CAS DataBase Reference)
• NIST Chemistry Reference: 8,8’-disulfanediylbis(N-benzylquinoline-3-carboxamide)(1414882-10-2)
• EPA Substance Registry System: 8,8’-disulfanediylbis(N-benzylquinoline-3-carboxamide)(1414882-10-2)

Safety Data

• Hazardous Substances Data: 1414882-10-2(Hazardous Substances Data)

Upstream product

• 1414882-17-9 8-(tert-butylthio)quinoline-3-carboxylic acid 
• 71082-53-6 8-fluoroquinoline-3-carboxylic acid 
• 1414882-25-9 8,8’-disulfanediylbis(quinoline-3-carboxylic acid) 
• 100-46-9 benzylamine 

Relevant articles and documents

Discovery of an Inhibitor of the Proteasome Subunit Rpn11

The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ～2.5 μM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ～400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.

COMPOSITIONS AND METHODS FOR JAMM PROTEIN INHIBITION

Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed.