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

ONX-0914 TFA (Synonyms: PR-957 TFA)

Cat. No.: HY-13207A
Handling Instructions

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

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

ONX-0914 TFA Chemical Structure

ONX-0914 TFA Chemical Structure

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Solution
10 mM * 1 mL USD 145 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of ONX-0914 TFA:

Top Publications Citing Use of Products

    ONX-0914 TFA 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 TFA 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 TFA 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.
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    Description

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

    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

    694.70

    Formula

    C₃₃H₄₁F₃N₄O₉

    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.O=C(O)C(F)(F)F

    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
    References
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    Keywords:

    ONX-0914PR-957ONX0914ONX 0914PR957PR 957ProteasomeBacterialHIVHuman immunodeficiency virusarthritisBALB/cmiceCAIACIALMP7cytokineprovirusInhibitorinhibitorinhibit

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    Product Name:
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