ONX-0914 (PR-957)

ONX-0914, also known as PR-957, is a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome. ONX-0914 selectively inhibits low-molecular mass polypeptide-7 (LMP7), the subunit specific for the immunoproteasome that catalyzes the chymotyrpsion-like activity, with an IC50 < 100 nM. Cell culture and animal studies have shown that ONX-0914 blocks the production of proinflammatory cytokines including interleukin-6 and 17, indicating that it has potential uses in the treatment of some autoimmune diseases such as rheumatoid arthritis, inflammatory bowel disease and lupus.

Dose: 0.1-0.5 μM for in vitro or cell couture assays; intravenous or subcutaneous administration at 2-10 mg/Kg daily for 5-7 days for animal studies.

Additional Information

Product Name: ONX-0914 (PR-957)
Also Known As: ONX 0914; ONX0914; ONX-0914; PR-957; CAS#: 960374-59-8
Catalog No.: F1410
Size: 5 mg
Molecular Weight: 580.7 Da
Species: N/A
Source: Synthetic
Stock: Powder
Concentration: N/A
Quality Assurance: >98% by HPLC and NMR
Storage: Eligible for room temperature shipping. Store at -20°C upon receiving; protect from air and ligh.
PDF Data Sheet: PDF Datasheet, MSDS
NCBI RefSeq: N/A
Image(s): No
Shipping Method: Room temperature shipping
References: 1. Muchamuel T, et al. (2009) Nat Med. 15(7):781-7.
2. Basler M, et al. (2010) J Immunol. 185(1):634-41.
3. Kalim KW, et al. (2012) J Immunol. 189(8):4182-93.

Details

ONX-0914, also known as PR-957, is a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome. ONX-0914 selectively inhibits low-molecular mass polypeptide-7 (LMP7), the subunit specific for the immunoproteasome that catalyzes the chymotyrpsion-like activity, with an IC50 < 100 nM. Cell culture and animal studies have shown that ONX-0914 blocks the production of proinflammatory cytokines including interleukin-6 and 17, indicating that it has potential uses in the treatment of some autoimmune diseases such as rheumatoid arthritis, inflammatory bowel disease and lupus.

Dose: 0.1-0.5 μM for in vitro or cell couture assays; intravenous or subcutaneous administration at 2-10 mg/Kg daily for 5-7 days for animal studies.