| 名称 | Oprozomib |
| 描述 | Oprozomib (PR-047) (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity. |
| 细胞实验 | MTT assay(Only for Reference) |
| 激酶实验 | 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. |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (174.6 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | apoptosis | inhibit | bioavailable | immunoproteasome LMP7 | PR047 | PR 047 | Proteasome | Autophagy | orally | ONX0912 | ONX-0912 | Inhibitor | epoxyketone | Oprozomib |
| 相关产品 | Stavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相关库 | 经典已知活性库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗肝癌化合物库 | 抗癌活性化合物库 | 抗癌药物库 |
United States
