ONX-0914 TFA (Synonyms: PR-957 TFA)

Name: ONX-0914 TFA
Brand: MedChemExpress
SKU: HY-13207A
Rating: 5.0 (17 reviews)

Cat. No.: HY-13207A Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

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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 (K_i=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

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 145	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	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
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of ONX-0914 TFA:

ONX-0914 In-stock

: ONX-0914 TFA 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 TFA 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 TFA 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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Description

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

694.70

Formula

C₃₃H₄₁F₃N₄O₉

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (143.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4395 mL	7.1974 mL	14.3947 mL
5 mM	0.2879 mL	1.4395 mL	2.8789 mL
10 mM	0.1439 mL	0.7197 mL	1.4395 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 (sealed storage, away from moisture). 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

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: ≥ 2.5 mg/mL (3.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

Dosing volume
(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.01%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (248 KB) HNMR (295 KB) LCMS (103 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	1.4395 mL	7.1974 mL	14.3947 mL	35.9868 mL
	5 mM	0.2879 mL	1.4395 mL	2.8789 mL	7.1974 mL
	10 mM	0.1439 mL	0.7197 mL	1.4395 mL	3.5987 mL
	15 mM	0.0960 mL	0.4798 mL	0.9596 mL	2.3991 mL
	20 mM	0.0720 mL	0.3599 mL	0.7197 mL	1.7993 mL
	25 mM	0.0576 mL	0.2879 mL	0.5758 mL	1.4395 mL
	30 mM	0.0480 mL	0.2399 mL	0.4798 mL	1.1996 mL
	40 mM	0.0360 mL	0.1799 mL	0.3599 mL	0.8997 mL
	50 mM	0.0288 mL	0.1439 mL	0.2879 mL	0.7197 mL
	60 mM	0.0240 mL	0.1200 mL	0.2399 mL	0.5998 mL
	80 mM	0.0180 mL	0.0900 mL	0.1799 mL	0.4498 mL
	100 mM	0.0144 mL	0.0720 mL	0.1439 mL	0.3599 mL

ONX-0914 TFA Related Classifications

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

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ONX-0914 TFA (Synonyms: PR-957 TFA)

Customer Review

Other Forms of ONX-0914 TFA:

ONX-0914 TFA Related Antibodies

14 Publications Citing Use of MCE ONX-0914 TFA

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References

Customer Review

ONX-0914 TFA Related Antibodies

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Complete Stock Solution Preparation Table

ONX-0914 TFA Related Classifications

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