ONX-0914 (Synonyms: PR-957)

Name: ONX-0914
Brand: MedChemExpress
SKU: HY-13207
Rating: 5.0 (18 reviews)

Cat. No.: HY-13207 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

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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 (K_i=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

CAS No. : 960374-59-8

Size	Price	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 192	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 192	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1180	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of ONX-0914:

ONX-0914 TFA Get quote

15 Publications Citing Use of MCE ONX-0914

: ONX-0914 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523. [Abstract]; 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.

: ONX-0914 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523. [Abstract]; 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 MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523. [Abstract]; 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.

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Biological Activity
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References
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Description

IC₅₀ & Target

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	EC₅₀	1.3 μM Compound: ONX-0914	Cytotoxicity against human Caco2 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human Caco2 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
Fibroblast	EC₅₀	0.16 μM Compound: ONX-0914	Cytotoxicity against human fibroblasts assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human fibroblasts assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
HCT-116	EC₅₀	0.11 μM Compound: ONX-0914	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
Huh-7	EC₅₀	0.39 μM Compound: ONX-0914	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
MCF7	EC₅₀	0.26 μM Compound: ONX-0914	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
MDA-MB-231	EC₅₀	0.27 μM Compound: ONX-0914	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
MM1.S	IC₅₀	0.24 μM Compound: 4; ONX-091	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 34087498]
NCI-H727	EC₅₀	0.3 μM Compound: ONX-0914	Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human NCI-H727 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
PBMC	IC₅₀	0.12 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-12/23 p40 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-12/23 p40 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	0.22 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced GMCSF production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced GMCSF production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	0.24 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	0.56 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNF-alpha production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNF-alpha production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	1.11 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	1.47 μM Compound: 3; ONX 0914; PR-957; LMP7	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced Il-1b production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced Il-1b production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs	[PMID: 28435528]
PBMC	IC₅₀	3.4 μM Compound: 3; ONX 0914; PR-957; LMP7	Cytotoxicity against human PBMC assessed as decrease in cell viability by CellTiter-Glo assay Cytotoxicity against human PBMC assessed as decrease in cell viability by CellTiter-Glo assay	[PMID: 28435528]
PC-3	EC₅₀	0.33 μM Compound: ONX-0914	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by Hoechst 33342 staining based HCS assay	[PMID: 29339252]
Raji	IC₅₀	> 10 μM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry	[PMID: 25006746]
Raji	IC₅₀	0.46 μM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry	[PMID: 25006746]
Raji	IC₅₀	0.59 μM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry	[PMID: 25006746]
Raji	IC₅₀	1.1 μM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-2c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry Inhibition of 20s proteasome subunit beta-2c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry	[PMID: 25006746]
Raji	IC₅₀	5.7 nM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-5i in human Raji cells using BODIPY-NC005 by fluorescent densitometry Inhibition of proteasome subunit beta-5i in human Raji cells using BODIPY-NC005 by fluorescent densitometry	[PMID: 25006746]
Raji	IC₅₀	54 nM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-5c in human Raji cells using BODIPY-NC005 by fluorescent densitometry Inhibition of 20s proteasome subunit beta-5c in human Raji cells using BODIPY-NC005 by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	> 5 μM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-1c in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry Inhibition of 20s proteasome subunit beta-1c in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	0.018 μM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-5i in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry Inhibition of proteasome subunit beta-5i in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	0.18 μM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-5c in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry Inhibition of 20s proteasome subunit beta-5c in human RPMI8226 cells using BODIPY-NC005 by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	0.34 μM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry Inhibition of proteasome subunit beta-1i in human RPMI8226 cells using BODIPY-NC001 by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	0.59 μM Compound: 1, ONX-0914	Inhibition of proteasome subunit beta-2i in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry Inhibition of proteasome subunit beta-2i in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry	[PMID: 25006746]
RPMI-8226	IC₅₀	0.68 μM Compound: 4; ONX-091	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 34087498]
RPMI-8226	IC₅₀	1.1 μM Compound: 1, ONX-0914	Inhibition of 20s proteasome subunit beta-2c in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry Inhibition of 20s proteasome subunit beta-2c in human RPMI8226 cells using BODIPY-epoxomicin by fluorescent densitometry	[PMID: 25006746]

In Vitro

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

MedChemExpress (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].

MedChemExpress (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.

960374-59-8

Appearance

Solid

Color

White to yellow

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

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.17 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (252 KB) HNMR (291 KB) LCMS (229 KB)

Handling Instructions (2659 KB)

References

[1]. Muchamuel T, et al. A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis [published correction appears in Nat Med. 2009 Nov;15(11):1333]. Nat Med. 2009;15(7):781-787. [Content Brief]

[2]. Rožman K, et al. Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome. Molecules. 2020;25(6):1305. Published 2020 Mar 12. [Content Brief]

[3]. Lin J, et al. PR-957, a selective immunoproteasome inhibitor, reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1. Biochem Pharmacol. 2018;156:511-523. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7221 mL	8.6107 mL	17.2215 mL	43.0537 mL
	5 mM	0.3444 mL	1.7221 mL	3.4443 mL	8.6107 mL
	10 mM	0.1722 mL	0.8611 mL	1.7221 mL	4.3054 mL
	15 mM	0.1148 mL	0.5740 mL	1.1481 mL	2.8702 mL
	20 mM	0.0861 mL	0.4305 mL	0.8611 mL	2.1527 mL
	25 mM	0.0689 mL	0.3444 mL	0.6889 mL	1.7221 mL
	30 mM	0.0574 mL	0.2870 mL	0.5740 mL	1.4351 mL
	40 mM	0.0431 mL	0.2153 mL	0.4305 mL	1.0763 mL
	50 mM	0.0344 mL	0.1722 mL	0.3444 mL	0.8611 mL
	60 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7176 mL

ONX-0914 Related Classifications

Inflammation/Immunology Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ONX-0914960374-59-8PR-957ONX0914ONX 0914PR957PR 957ProteasomeBacterialHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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ONX-0914 (Synonyms: PR-957)

Customer Review

Other Forms of ONX-0914:

ONX-0914 Related Antibodies

15 Publications Citing Use of MCE ONX-0914

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All HIV Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ONX-0914 Related Antibodies

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Complete Stock Solution Preparation Table

ONX-0914 Related Classifications

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