1. Metabolic Enzyme/Protease
    Anti-infection
  2. Proteasome
    Bacterial
    HIV
  3. ONX-0914

ONX-0914 (Synonyms: PR-957)

Cat. No.: HY-13207 Purity: 99.72%
Handling Instructions

ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.

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
Solution
10 mM * 1 mL in DMSO USD 133 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 133 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 105 In-stock
Estimated Time of Arrival: December 31
10 mg USD 176 In-stock
Estimated Time of Arrival: December 31
50 mg USD 429 In-stock
Estimated Time of Arrival: December 31
100 mg USD 715 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of ONX-0914:

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

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    • Customer Review

    Description

    ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1[1][2][3].

    IC50 & Target

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

    In Vitro

    ONX-0914 inhibits LMP7-specific antigen presentation. ONX-0914 blocks cytokine productionby mouse splenocytes and blocks T celldifferentiation[1].

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

    In Vivo

    ONX-0914 (2-10 mg/kg; i.v,; on days 4, 6 and 8) meliorates disease in mouse arthritis[1].
    ONX-0914 (2, 6 and 10 mg per kg body weight on days 25, 27, 29, 31 and 33; i.v.) treatment also induced a rapid therapeutic response in the T and B cell–dependent CIA (collagen-induced arthritis) model[1].

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

    Animal Model: Collagen antibody-induced arthritis (CAIA, Arthritis was induced in BALB/c mice with antibodies specific for type II collagen (mAb) and endotoxin)[1]
    Dosage: 2, 6 or 10 mg per kg body weight
    Administration: I.v.; treated on days 4, 6 and 8
    Result: Blocked disease progression in a dose-dependent manner and completely ameliorated visible signs of disease at the highest dose.
    Molecular Weight

    580.67

    Formula

    C31H40N4O7

    CAS No.
    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 available by MCE.
    References

    Purity: 99.72%

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