2. Metabolic Enzyme/Protease Apoptosis
  3. Proteasome Apoptosis
  4. PR-924

PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.

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PR-924 Chemical Structure

PR-924 Chemical Structure

CAS No. : 1416709-79-9

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Solid + Solvent
10 mM * 1 mL in DMSO
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5 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

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PR-924 Related Antibodies

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Description

PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities[1][2].

IC50 & Target

IC50: 22 nM (LMP7), 8.2 μM (LMP2)[2]
In Vitro

PR-924 (1-20 μM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells) treatment significantly decreases the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h)[1].
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells[1].
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels[1].
PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release[1].

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

PR-924 Related Antibodies

Cell Viability Assay[1]

Cell Line: MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells
Concentration: 1-20 μM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Significantly decreased the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h).

Apoptosis Analysis[1]

Cell Line: MM.1S and MM.1R cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Triggered a significant increase in the Annexin V+/PI-apoptotic cell population.

Western Blot Analysis[1]

Cell Line: MM.1S and MM.1R cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Triggered activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein.
In Vivo

PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts[1].
PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival[1].

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

Animal Model: CB-17 SCID-mice injected with MM.1S cells[1]
Dosage: 6 mg/kg
Administration: Intravenous injection; twice a week; for 21 days
Result: Inhibited tumour growth in human plasmacytoma xenografts.
Molecular Weight

618.72

Formula

C37H38N4O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N[C@@H](CC1=CC=CC=C1)C([C@]2(CO2)C)=O)[C@@H](NC([C@@H](C)NC(C(CC3=CC=CC=C43)=C4C)=O)=O)CC5=CNC6=CC=CC=C56
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 : 50 mg/mL (80.81 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 1.6162 mL 8.0812 mL 16.1624 mL
5 mM 0.3232 mL 1.6162 mL 3.2325 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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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 (4.04 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.04 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:

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6162 mL 8.0812 mL 16.1624 mL 40.4060 mL
5 mM 0.3232 mL 1.6162 mL 3.2325 mL 8.0812 mL
10 mM 0.1616 mL 0.8081 mL 1.6162 mL 4.0406 mL
15 mM 0.1077 mL 0.5387 mL 1.0775 mL 2.6937 mL
20 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
25 mM 0.0646 mL 0.3232 mL 0.6465 mL 1.6162 mL
30 mM 0.0539 mL 0.2694 mL 0.5387 mL 1.3469 mL
40 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0102 mL
50 mM 0.0323 mL 0.1616 mL 0.3232 mL 0.8081 mL
60 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6734 mL
80 mM 0.0202 mL 0.1010 mL 0.2020 mL 0.5051 mL
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PR-924 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:

PR-9241416709-79-9PR924PR 924ProteasomeApoptosisLMP-7tripeptideepoxyketonecovalentlyN-terminalthreonineshIL-6Rβ5imitochondriaantitumorapoptosisInhibitorinhibitorinhibit

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