Oprozomib

SKU: orb1301126

Description

Oprozomib (ONX 0912) is an orally bioavailable proteasome inhibitor that selectively targets the CT-L activity of the 20S proteasome subunits β5 (IC50=36 nM) and LMP7 (IC50=82 nM). It exhibits antineoplastic activity and has been investigated in preclinical in vitro and in vivo studies for hematological malignancies and solid tumors.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 935888-69-0
• MW: 532.61
• Purity: 99.87% (May vary between batches)
• Formula: C₂₅H₃₂N₄O₇S
• SMILES: COC[C@H](NC(=O)[C@H](COC)NC(=O)c1cnc(C)s1)C(=O)N[C@@H](Cc1ccccc1)C(=O)[C@@]1(C)CO1
• Target: Autophagy,Proteasome,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.2 mM);DMSO:93 mg/mL (174.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  20S proteasome β5:36 nM|20S proteasome LMP7:82 nM
• In Vivo:
  Oprozomib exhibits anti-MM (multiple myeloma) activity by inhibiting the migration and angiogenesis of MM cells. Furthermore, Oprozomib suppresses the activation of caspase-8, caspase-9, caspase-3, and PARP.
• In Vitro:
  In various human tumor xenografts and mouse syngeneic models, Oprozomib can inhibit over 80% of proteasomes, inducing an anti-tumor response. Following repeated oral administration, Oprozomib demonstrates good safety and tolerability across most tissues in animals.
• Cell Research:
  MTT assay(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

orally, Oprozomib, ONX 0912, ONX0912, ONX-0912, immunoproteasome LMP7, inhibit, Inhibitor, epoxyketone, bioavailable, apoptosis, Autophagy, 20S proteasome, PR047, PR-047, PR 047, Proteasome

Compound Identifiers

PubChem CID

25067547