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ProductsBack/ONX 0914 [960374-59-8]
Chemical Structure
Chemical Structure
Chemical Structure

ONX 0914 [960374-59-8]

Research Use Only
AG-CR1-3674
AdipoGen Life Sciences
CAS Number960374-59-8
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight580.7
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    ONX 0914 [960374-59-8]
  • Delivery Days Customer
    10
  • CAS Number
    960374-59-8
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Hazard Information
    Warning
  • Molecular Formula
    C31H40N4O7
  • Molecular Weight
    580.7
  • Scientific Description
    Chemical. CAS: 960374-59-8. Formula: C31H40N4O7. MW: 580.7. Synthetic. Potent and selective 20S immunoproteasome inhibitor. Targets the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=73nM) and with minimal crossreactivity to the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=1.04microM). Potent anti-inflammatory and anticancer agent. Inhibits production of pro-inflammatory cytokines and can induce apoptosis in vitro. Inhibits presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo, which consequently blocks production of interleukin-23 (IL-23) by activated monocytes and IFN-gamma and IL-2 by T cells. Can also inhibit IL-17-producing T cells under TH17-polarizing conditions in vitro and reduce TH1 and TH17 cell differentiation in vivo. Shown to attenuate disease progression in several experimental models of autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus, as well as in some hematologic malignancies and other cancer types. - Potent and selective 20S immunoproteasome inhibitor. Targets the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=73nM) and with minimal cross-reactivity to the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=1.04microM). Potent anti-inflammatory and anticancer agent. Inhibits production of pro-inflammatory cytokines and can induce apoptosis in vitro. Inhibits presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo, which consequently blocks production of interleukin-23 (IL-23) by activated monocytes and IFN-gamma and IL-2 by T cells. Can also inhibit IL-17-producing T cells under TH17-polarizing conditions in vitro and reduce TH1 and TH17 cell differentiation in vivo. Shown to attenuate disease progression in several experimental models of autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus, as well as in some hematologic malignancies and other cancer types.
  • SMILES
    O=C(N[C@@H](C)C(N[C@@H](CC1=CC=C(OC)C=C1)C(N[C@@H](CC2=CC=CC=C2)C([C@]3(C)OC3)=O)=O)=O)CN4CCOCC4
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis: T. Muchamuel, et al.; Nat. Med. 15, 781 (2009)
  • Prevention of experimental colitis by a selective inhibitor of the immunoproteasome: M. Basler, et al.; J. Immunol. 185, 634 (2010)
  • Immunoproteasome-specific inhibitors and their application: M. Basler & M. Groettrup; Methods Mol. Biol. 832, 391 (2012)
  • Prophylactic and therapeutic efficacies of a selective inhibitor of the immunoproteasome for Hashimoto's thyroiditis, but not for Graves' hyperthyroidism, in mice: Y. Nagayama, et al.; Clin. Exp. Immunol. 168, 268 (2012)
  • Immunoproteasome subunit LMP7 deficiency and inhibition suppresses Th1 and Th17 but enhances regulatory T cell differentiation: K.W. Kalim, et al.; J. Immunol. 189, 4182 (2012)
  • Inhibition of the immunoproteasome ameliorates experimental autoimmune encephalomyelitis: M. Basler, et al.; EMBO Mol. Med. 6, 226 (2014)
  • Interferon-gamma-induced upregulation of immunoproteasome subunit assembly overcomes bortezomib resistance in human hematological cell lines: D. Niewerth, et al.; J. Hematol. Oncol. 7, 7 (2014)
  • Bortezomib-resistant mutant proteasomes: structural and biochemical evaluation with carfilzomib and ONX 0914: E.M. Huber, et al.; Structure 23, 407 (2015)
  • Inhibition of the Immunoproteasome Subunit LMP7 with ONX 0914 Ameliorates Graft-versus-Host Disease in an MHC-Matched Minor Histocompatibility Antigen-Disparate Murine Model: J. Zilberberg, et al.; Biol. Blood Marrow Transplant 21, 1555 (2015)
  • PR-957, a selective inhibitor of immunoproteasome subunit low-MW polypeptide 7, attenuates experimental autoimmune neuritis by suppressing Th17-cell differentiation and regulating cytokine production: H. Liu, et al.; FASEB J. 31, 1756 (2017)