ONX-0914 (PR-957)

For research use only.

Catalog No.S7172

14 publications

ONX-0914 (PR-957) Chemical Structure

CAS No. 960374-59-8

ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.

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Selleck's ONX-0914 (PR-957) has been cited by 14 publications

2 Customer Reviews

  • Dependence of SPRI signal on receptor concentration: (a) ONX 0914 inhibitor, (b) inhibitor 5. 20Si concentration: 2.8 μg/mL, pH 7.4

    Cell Mol Bioeng, 2017, 10(2):174-185. ONX-0914 (PR-957) purchased from Selleck.

  • Mice were treated with daily doses of 10 mg/kg ONX-0914 iv or vehicle (n = 5–6). Not significant by log-rank test.

    Parasite Immunol, 2015, 37(11):599-604.. ONX-0914 (PR-957) purchased from Selleck.

Purity & Quality Control

Choose Selective Proteasome Inhibitors

Biological Activity

Description ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay.
Features The first highly selective, small molecule inhibitor of the immunoproteasome. Potential use in cancer and autoimmune diseases (e.g. rheumatoid arthritis, inflammatory bowel disease, and lupus).
Targets
LMP7 [1]
(Cell-free assay)
~10 nM
In vitro

ONX-0914 is 20- to 40-fold more selective for LMP7 over the next most sensitive sites, β5 or LMP2. ONX-0914 blocks presentation of LMP7-specific, MHC-I–restricted antigens in vitro and in vivo with minimal cross-reactivity for the constitutive proteasome. Selective inhibition of LMP7 by ONX-0914 blocks production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells. LMP7 inhibition blocks production of IL-23 by ~90% and of tumor necrosis factor-α (TNF-α) and IL-6 by ~50%.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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SJ-GBM2 MVnxTHRUKGG|c3H5 NEnjW2VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> M4LSZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEC2O|Q3Lz5{NUCwOlc1PjxxYU6=
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Raji NVjWWGtTTnWwY4Tpc44h[XO|YYm= NXzhR212UW6qaXLpeIlwdiCxZjDwdo91\WG|b33lJJN2[nWwaYSgZoV1[S1zaTDpckBpfW2jbjDSZYpqKGOnbHzzJJV{cW6pIFLPSGlRYS1iZYDvfI9ucWOrbjDifUBndHWxcnXzZ4VvfCCmZX7zbZRwdWW2comsJGlEPTB;MD60Ou69VQ>? Mn73QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyME[3OFYoRjJ3MEC2O|Q3RC:jPh?=
Raji NYjQUJhHTnWwY4Tpc44h[XO|YYm= NGTvWlJKdmirYnn0bY9vKG:oIIDyc5Rm[XOxbXWgd5VjfW6rdDDi[ZRiNTKrIHnuJIh2dWGwIGLhbokh[2WubIOgeZNqdmdiQl;ETXB[NSCncH;4c41q[2mwIHL5JIZtfW:{ZYPj[Y51KGSnboPpeI9u\XS{eTygTWM2OD1yLkW5{txO MojKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyME[3OFYoRjJ3MEC2O|Q3RC:jPh?=
RPMI8226 NIDBOIhHfW6ldHnvckBie3OjeR?= NV2y[ZRnUW6qaXLpeIlwdiCxZjDwdo91\WG|b33lJJN2[nWwaYSgZoV1[S1{aTDpckBpfW2jbjDSVG1KQDJ{NjDj[YxteyC3c3nu[{BDV0SLUGmt[ZBwgG:vaXPpckBjgSCobIXvdoV{[2WwdDDk[Y5{cXSxbXX0dpktKEmFNUC9NE42Qc7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTByNke0Okc,OjVyME[3OFY9N2F-
Raji M4PFSGZ2dmO2aX;uJIF{e2G7 NEflT5lKdmirYnn0bY9vKG:oIEKwd{Bxem:2ZXHzc41mKHO3YoXubZQh[mW2YT2yZ{BqdiCqdX3hckBT[WqrIHPlcIx{KHW|aX7nJGJQTEmSWT2g[ZBwgG:vaXPpckBjgSCobIXvdoV{[2WwdDDk[Y5{cXSxbXX0dpktKEmFNUC9NU4y|ryP MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTByNke0Okc,OjVyME[3OFY9N2F-
RPMI8226 MkjYSpVv[3Srb36gZZN{[Xl? M13tdWlvcGmkaYTpc44hd2ZiMkDzJJBzd3SnYYPvcYUhe3WkdX7peEBj\XSjLULjJIlvKGi3bXHuJHJRVUl6MkK2JINmdGy|IIXzbY5oKEKRRFnQXU1meG:6b33pZ4lvKGK7IH\seY9z\XOlZX70JIRmdnOrdH;t[ZRzgSxiSVO1NF0yNjIQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTByNke0Okc,OjVyME[3OFY9N2F-
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RD NH[0dFNyUFSVIHHzd4F6 MliydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NHzTc3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOzPVI2Oid-MkmzN|kzPTJ:L3G+
MG 63 (6-TG R) Ml:5dWhVWyCjc4PhfS=> NVH6epVseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M2\EWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{O5NlUzLz5{OUOzPVI2OjxxYU6=
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MOLT4 NI\mcVVHfW6ldHnvckBie3OjeR?= MkDGTY5pcWKrdHnvckBw\iCPRVPMNUBqdiCqdX3hckBOV0yWNDDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjlyMt88US=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN6MEi2N{c,OzB|OEC4OlM9N2F-
A20 MmHYSpVv[3Srb36gZZN{[Xl? MnTDTY5pcWKrdHnvckBw\iB{MGOgdJJwfGWxc3;t[UBj\XSjIEKgbY4hdW:3c3WgRVIxKGOnbHzzJIJ6KEWOSWPBMEBKSzVyPUCuPVE{|ryP M1KyOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{iwPFY{Lz5|MEO4NFg3OzxxYU6=
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... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: collagen antibody–induced arthritis (CAIA) and collagen-induced arthritis (CIA)
  • Dosages: 2, 6 or 10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.21 mM)
Ethanol 100 mg/mL (172.21 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+castor oil
For best results, use promptly after mixing.
10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 580.67
Formula

C31H40N4O7

CAS No. 960374-59-8
Storage powder
in solvent
Synonyms N/A
Smiles CC(C(=O)NC(CC1=CC=C(C=C1)OC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C)NC(=O)CN4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID