ONX 0914

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ONX 0914

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Cat No: 16271

Biochemicals - Small Molecule Inhibitors

The immunoproteasome is a specialized, inducible proteasome that generates peptides presented on major histocompatibility complex (MHC) class I molecules to cytotoxic T cells. Stimulation of cells with inflammatory cytokines such as IFN-γ leads to the ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-?[2-?(4-?morpholinyl)?acetyl]?-?L-?alanyl-?O-?methyl-?N-?[(1S)?-?2-?[(2R)?-?2-?methyl-?2-?oxiranyl]?-?2-?oxo-?1-?(phenylmethyl)?ethyl]?-L-tyrosinamide

Correlated keywords:

1161839-?04-?8 LMP7 immunoproteasome T cell inflammatory cytokine immunology ?1i inhibitor autoimmune disease ONX0914 inhibit biochemical ubiquitin-proteasome ?5i LMP7 ?-5i LMP-7 subunit mouse human block production IL-23 IL23 monocyte IFN-? IFN? IL-2 IL2 IL-17-producing IL17 TH17-polarizing condition in vitro TH-17 TH1 TH-1 differentiation vivo attenuate progression experimental model hematologic malignancies specialized inducible proteasome peptide histocompatibility complex MHC class I molecule cytotoxic replacement constitutive catalytic production restricted epitope

Product Overview:
The immunoproteasome is a specialized, inducible proteasome that generates peptides presented on major histocompatibility complex (MHC) class I molecules to cytotoxic T cells. Stimulation of cells with inflammatory cytokines such as IFN-γ leads to the replacement of constitutive catalytic proteasome β subunits with inducible β subunits (β1i (LMP2), β2i (MECL1), and β5i (LMP7)), which are required for the production of certain MHC class I-restricted T cell epitopes. ONX 0914 is a selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) and demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse and human, respectively).{28373,28369} It can block the production of IL-23 by activated monocytes and the production of IFN-γ and IL-2 by T cells.{28373} ONX 0914 can also inhibit IL-17-producing T cells under TH17-polarizing conditions in vitro and reduce TH1 and TH17 cell differentiation in vivo.{28372} This compound has been shown to attenuate disease progression in several experimental models of autoimmune disorders as well as in some hematologic malignancies.{28373,28370,28241,28371}

Size	1 mg
Shipping	dry ice
CAS Number	960374-59-8
Molecular Formula	C₃₁H₄₀N₄O₇
SMILES	O=C([C@]1(C)OC1)[C@@H](NC([C@H](CC2=CC=C(OC)C=C2)NC([C@H](C)NC(CN3CCOCC3)=O)=O)=O)CC4=CC=CC=C4
Molecular Weight	580,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.