A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human

ONX 0914 – 5 mg

Brand:
Cayman
CAS:
960374-59-8
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse and human, respectively); blocks the production of proinflammatory cytokines and inhibits TH1 and TH17 cell differentiation; attenuates disease progression in several experimental models of autoimmune disorders as well as in some hematologic malignancies

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

Synonyms:  PR-957

Molecular weight: 580.7

CAS: 960374-59-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity

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