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Oprozomib (ONX 0912, PR-047) is an orally bioavailable and selective proteasome inhibitor. Oprozomib (ONX 0912) selectively inhibited CT-L activity of both the constitutive proteasome (beta5) and immunoproteasome (LMP7) and demonstrated an absolute bioavailability of up to 39% in rodents and dogs. Oprozomib inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. The anti-MM activity of Oprozomib (ONX 0912) is associated with activation of caspase-8, caspase-9, caspase-3, and poly(ADP) ribose polymerase, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib significantly reduced tumor progression and prolonged survival in animal tumor model studies. Immununostaining of MM tumors from ONX 0912-treated mice showed growth inhibition, apoptosis, and a decrease in associated angiogenesis. Finally, Oprozomib (ONX 0912) enhances anti-MM activity of bortezomib, lenalidomide dexamethasone, or pan-histone deacetylase inhibitor.
| Molecular Weight | 532.61 |
| Formula | C25H32N4O7S |
| CAS Number | 935888-69-0 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Proteasome Products |
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Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
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| ITMN-191
ITMN-191 (Danoprevir, RG7227) is a potent and orally active inhibitor of hepatitis C virus (HCV) NS3/4A serine protease with an IC50 of 1.6 nM. |
| MG132
MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132 is also a calpain inhibitor with IC50 of 1.2 μM. |
| IU1
IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
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