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Gamma Secretase

ONX0914 (PR-957) (960374-59-8)

ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.

Not Intended for Therapeutic Use. For research use only.

CAS: 960374-59-8 Category

ONX0914 (PR-957) (960374-59-8) Description:

ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease, and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome. Recent evidence suggests that the immunoproteasome regulates the production of several inflammatory cytokines, including Tumor Necrosis Factor-α (TNF-α), Interleukin-6 (IL-6), IL-17, and IL-23. In preclinical models of rhematoid arthritis and lupus, ONX 0914 blocked progression of these diseases at well-tolerated doses. Preclinical studies are underway to evaluate the potential of ONX 0914 in the treatment of a range of autoimmune disorders.

ONX0914 (PR-957) (960374-59-8) Specifications:

Product Name ONX-0914
Synonyms ONX 0914; ONX0914; ONX-0914; PR957; PR-957; PR 957
Chemical Names (S)-3-(4-methoxyphenyl)-N-((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 960374-59-8
Molecular Formula C31H40N4O7
Molecular Weight 580.67
Monoisotopic Mass 580.29 g/mol
MDL number MFCD26794217
InChIKey WQAVPPWWLLVGFK-VTNASVEKSA-N
InChi Code InChI=1S/C31H40N4O7/c1-21(32-27(36)19-35-13-15-41-16-14-35)29(38)34-26(18-23-9-11-24(40-3)12-10-23)30(39)33-25(28(37)31(2)20-42-31)17-22-7-5-4-6-8-22/h4-12,21,25-26H,13-20H2,1-3H3,(H,32,36)(H,33,39)(H,34,38)/t21-,25-,26-,31+/m0/s1
SMILES O=C(N[[email protected]@H](CC1=CC=CC=C1)C([[email protected]]2(C)OC2)=O)[[email protected]@H](NC([[email protected]@H](NC(CN3CCOCC3)=O)C)=O)CC4=CC=C(OC)C=C4
Form Powder
Color white to off-white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome with minimal cross-reactivity for the constitutive proteasome.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Eleftheriadis T, Pissas G, Antoniadi G, Liakopoulos V, Stefanidis I. Proteasome or immunoproteasome inhibitors cause apoptosis in human renal tubular epithelial cells under normoxic and hypoxic conditions. Int Urol Nephrol. 2016 Feb 26. [Epub ahead of print] PubMed PMID: 26920131.
  • 2: Mundt S, Basler M, Buerger S, Engler H, Groettrup M. Inhibiting the immunoproteasome exacerbates the pathogenesis of systemic Candida albicans infection in mice. Sci Rep. 2016 Jan 18;6:19434. doi: 10.1038/srep19434. PubMed PMID: 26776888; PubMed Central PMCID: PMC4726078.
  • 3: Walker-Caulfield ME, Guo Y, Johnson RK, McCarthy CB, Fitz-Gibbon PD, Lucchinetti CF, Howe CL. NFκB signaling drives pro-granulocytic astroglial responses to neuromyelitis optica patient IgG. J Neuroinflammation. 2015 Sep 30;12:185. doi: 10.1186/s12974-015-0403-8. PubMed PMID: 26423139; PubMed Central PMCID: PMC4590277.
  • 4: Howland SW, Ng GX, Chia SK, Rénia L. Investigating proteasome inhibitors as potential adjunct therapies for experimental cerebral malaria. Parasite Immunol. 2015 Nov;37(11):599-604. doi: 10.1111/pim.12277. PubMed PMID: 26366636.
  • 5: Zhang HM, Fu J, Hamilton R, Diaz V, Zhang Y. The mammalian target of rapamycin modulates the immunoproteasome system in the heart. J Mol Cell Cardiol. 2015 Sep;86:158-67. doi: 10.1016/j.yjmcc.2015.07.027. Epub 2015 Aug 1. PubMed PMID: 26239133.