Oprozomib

Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells[1].

Product Specifications

CAS Number

[935888-69-0]

Product Name Alternative

ONX 0912; PR-047

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; Proteasome

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Oprozomib.html

Purity

99.76

Solubility

DMSO : ≥ 50 mg/mL

Smiles

C[C@]1(OC1)C([C@H](CC2=CC=CC=C2)NC([C@@H](NC([C@@H](NC(C3=CN=C(C)S3)=O)COC)=O)COC)=O)=O

Molecular Formula

C25H32N4O7S

Molecular Weight

532.61

Precautions

H302, H315, H319, H335

References & Citations

[1]Han-Jie Zhou, et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047) . J Med Chem. 2009 May 14;52 (9) :3028-38.|[2]Dharminder Chauhan, et al. A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood. 2010 Dec 2;116 (23) :4906-15.|[3]M A Hurchla, et al.The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects. Leukemia. 2013 Feb;27 (2) :430-40.