1. Metabolic Enzyme/Protease
  2. Proteasome
  3. ONX-0914

ONX-0914 (Synonyms: PR-957)

Cat. No.: HY-13207 Purity: 98.86%
Handling Instructions

ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome subunit LMP7.

For research use only. We do not sell to patients.

ONX-0914 Chemical Structure

ONX-0914 Chemical Structure

CAS No. : 960374-59-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 270 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ONX-0914 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.

    The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

    ONX-0914 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.

    Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.

    ONX-0914 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.

    J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 µM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    ONX-0914 (PR-957) is a potent and selective inhibitor of immunoproteasome subunit LMP7.

    IC50 & Target

    IC50: ~10 nM (LMP7)[1].

    In Vitro

    PR-957 blocked presentation of LMP7-specific, MHC-I-restricted antigens in vitro and in vivo. Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells[1].

    In Vivo

    In mouse models of rheumatoid arthritis and lupus, ONX-0914 treatment reverses signs of disease and results in reductions in cellular infiltration, cytokine production and autoantibody levels at well-tolerated doses. The maximum tolerated dose (MTD) of ONX-0914 in mice to be 30 mg/kg body weight. IFN-g release is inhibited by ~60% at LMP7-selective concentrations of ONX-0914 and by ~90% at higher concentrations. Production of IL-2 is also inhibited by ~50%[1].

    Molecular Weight

    580.67

    Formula

    C₃₁H₄₀N₄O₇

    CAS No.

    960374-59-8

    SMILES

    O=C(N[[email protected]@H](C)C(N[[email protected]@H](CC1=CC=C(OC)C=C1)C(N[[email protected]@H](CC2=CC=CC=C2)C([[email protected]]3(C)OC3)=O)=O)=O)CN4CCOCC4

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (60.28 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7221 mL 8.6107 mL 17.2215 mL
    5 mM 0.3444 mL 1.7221 mL 3.4443 mL
    10 mM 0.1722 mL 0.8611 mL 1.7221 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.17 mg/mL (3.74 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.17 mg/mL (3.74 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.17 mg/mL (3.74 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay

    Stock solutions of PR-957 was prepared in DMSO and were diluted 400-fold for cell treatments. Drug treatments were performed in RPMI-1640 media containing 5% FBS, 100 units/ml penicillin and 100 μg/ml streptomycin. Cells were exposed to PR-957 or 0.25% DMSO at 37°C for a 1 hr period followed by four washes with media (RPMI-1640 containing 5% FBS) prior to either stimulation or washing [twice with media and twice with phosphate buffered saline (PBS)], lysis in hypotonic TE buffer (20 mM Tris HCL and 5 mM EDTA pH 8.0), and storage at -80°C for the active site ELISA. Tissue culture media and fetal bovine serum (FBS) were purchased from Mediatech or Invitrogen-Life Technologies.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.86%

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    Keywords:

    ONX-0914PR-957ONX0914ONX 0914PR957PR 957ProteasomeInhibitorinhibitorinhibit

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    Product name:
    ONX-0914
    Cat. No.:
    HY-13207
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