Oprozomib [ONX 0912]

Synthetic. Chemical. CAS: 935888-69-0. Formula: C25H32N4O7S. MW: 532.6. Synthetic. Potent orally bioavailable irreversible proteasome inhibitor. Analog of Carfilzomib (AG-CR1-3669). Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=36nM) and the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=82nM). Anticancer compound effective in cell-based assays, in xenografts and against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, as well as in bortezomib resistant multiple myeloma cells. Shown to have anti-angiogenic activity. Has potential applications in certain types of cancer as well as other diseases that require proteasome activity.