PR-924
Based on 1 Customer Validation
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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- Pureza: 98.87%
- No. CAS: 1416709-79-9
- Fòrmula: C37H38N4O5
- Peso molecular:618.72
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 22 nM (LMP7), 8.2 μM (LMP2)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Raji | IC50 |
>10 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| Raji | IC50 |
>10 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| Raji | IC50 |
>10 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| Raji | IC50 |
1.84 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| Raji | IC50 |
2.5 nM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| Raji | IC50 |
227 nM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
>100 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
>100 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
>100 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
0.025 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
2.9 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
| RPMI-8226 | IC50 |
3.5 μM
Compound: 2, PR-924
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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
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[PMID: 25006746] |
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.
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Cell Line:MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells
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Concentration:1-20 μM
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Incubation Time:24 hours, 48 hours, and 72 hours
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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).
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Cell Line:MM.1S and MM.1R cells
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Concentration:3 μM
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Incubation Time:48 hours
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Result:Triggered a significant increase in the Annexin V+/PI-apoptotic cell population.
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Cell Line:MM.1S and MM.1R cells
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Concentration:3 μM
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Incubation Time:48 hours
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Result:Triggered activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein.
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.
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Animal Model:CB-17 SCID-mice injected with MM.1S cells[1]
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Dosage:6 mg/kg
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Administration:Intravenous injection; twice a week; for 21 days
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Result:Inhibited tumour growth in human plasmacytoma xenografts.
Chemical Information
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No. CAS 1416709-79-9
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Appearance Solid
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Peso molecular 618.72
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Fòrmula C37H38N4O5
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Singh AV, et al. PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo. Br J Haematol. 2011 Jan;152(2):155-63. [Content Brief]
[2]. Parlati F, et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. Blood. 2009 Oct 15;114(16):3439-47. [Content Brief]
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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