CEP-7055 - CAS 402857-58-3

CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB.

Others, VEGFR

Tyrosine Kinase/Adaptors, Others, Angiogenesis

402796

C32H35N3O4

525.64

C(CCOC(CN(C)C)=O)N1C=2C(=C3C(=C4C2CC=5C4=CC=CC5)C(=O)NC3)C=6C1=CC=C(COC(C)C)C6

-20°C

Ice Packs

Small Compound