Oprozomib (ONX 0912)
Molecular Weight(MW): 532.61
Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
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The oprozomib-mediated inhibition of 20S proteasome activity exhibits slow-binding kinetics. (A) The effect of varying concentrations of oprozomib on the relative fluorescence increase due to the 20S proteasome-catalyzed hydrolysis of Suc-LLVY-AMC. Otherwise experimental conditions and comments are as in Fig. 3A above. (B) Plot of the pseudo-first order rate constant kobs calculated from curve fitting of progress curves to an equation describing slow-binding kinetics vs. the oprozomib concentration for the oprozomib-mediated inhibition of 20S proteasome activity. The solid straight line was linear-least squares calculated and yielded an apparent second order rate constant kon of (3.8 ± 0.2) × 103 M−1·s−1 from the slope. The calculated intercept was zero within its SE, consistent with slow-binding irreversible inhibition.
Archives of Biochemistry and Biophysics, 2018, 639:52-58. Oprozomib (ONX 0912) purchased from Selleck.
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|Description||Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.|
The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. 
|In vivo||Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models .|
ELISA-based active site binding assay:Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells.
|In vitro||DMSO||100 mg/mL (187.75 mM)|
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