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Oprozomib

Catalog No. T6041 CAS 935888-69-0

Synonyms: PR-047, ONX 0912

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.

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Oprozomib, CAS 935888-69-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 58.00
5 mg	In stock	$ 129.00
10 mg	In stock	$ 173.00
25 mg	In stock	$ 312.00
50 mg	In stock	$ 468.00
100 mg	In stock	$ 657.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 99.87%

Purity: 99.05%

Purity: 98%

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Storage & Solubility Information

Description	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.
Targets&IC50	20S proteasome β5:36 nM, 20S proteasome LMP7:82 nM
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.
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.
Kinase Assay	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.
Cell Research	MTT assay(Only for Reference)

Synonyms	PR-047, ONX 0912
Molecular Weight	532.61
Formula	C25H32N4O7S
CAS No.	935888-69-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (174.6 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Zhou HJ, et al. J Med Chem, 2009, 52(9), 3028-3038. 2. Chauhan D, et al. Blood, 2010, 116(23), 4906-4915. 3. Muchamuel T, Nat Med, 2009, 15(7), 781-787.

Citations

1. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326. 2. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Metabolism Disease Compound Library Protease Inhibitor Library HIF-1 Signaling Pathway Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library

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Keywords

Oprozomib 935888-69-0 Autophagy Proteases/Proteasome Ubiquitination Proteasome apoptosis inhibit bioavailable immunoproteasome LMP7 PR-047 PR047 PR 047 orally ONX0912 ONX-0912 Inhibitor epoxyketone ONX 0912 inhibitor

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