346640-08-2

Usage

Uses

Used in Pharmaceutical Research:
CCF-642 is used as a PDI inhibitor for studying its effects on reducing ER stress markers and neuroinflammation in the hippocampus of experimental autoimmune encephalomyelitis (EAE) mice. This application is significant as it helps researchers understand the potential therapeutic benefits of CCF-642 in treating conditions associated with ER stress and neuroinflammation.
Used in Neurological Applications:
In the field of neurology, CCF-642 is used as a PDI inhibitor to investigate its potential in mitigating neuroinflammation and ER stress in various neurological disorders. By reducing these markers, CCF-642 may contribute to the development of novel treatments for conditions such as multiple sclerosis, Alzheimer's disease, and other neurodegenerative diseases.
Used in Drug Development:
CCF-642 is also used in the development of new drugs targeting PDI, which plays a crucial role in protein folding and redox regulation. By inhibiting PDI, CCF-642 may help in the development of therapeutic agents that can modulate protein folding and redox processes, potentially leading to the treatment of various diseases and conditions.

Biochem/physiol Actions

CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. CCF642 displays anti-multiple myeloma (MM) activity both in cultures in vitro (IC50 <1 μM against murine 5TGM1 and nine human MM lines) and in mice in vivo (10 mg/kg, 3X i.p. per wk) without apparent adverse effects to the animals or being cytotoxic to normal bone marrow (NLBM) cells even at concentrations as high as 6.75 μM. Consistent with PDI′s role in ER protein folding process, CCF642 treatment causes acute ER stress accompanied by apoptosis-inducing calcium release in MM cells.