Art. -Nr.: HY-123587

PR-924

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.87%
CAS. Nr.: 1416709-79-9
Formel: C₃₇H₃₈N₄O₅
Molecular Weight:618.72

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PR-924 Chemical Structure

CAS. Nr.: 1416709-79-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 22 nM (LMP7), 8.2 μM (LMP2)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Raji	IC₅₀	>10 μM Compound: 2, PR-924	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	>10 μM Compound: 2, PR-924	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	>10 μM Compound: 2, PR-924	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	1.84 μM Compound: 2, PR-924	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	2.5 nM Compound: 2, PR-924	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	227 nM Compound: 2, PR-924	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	>100 μM Compound: 2, PR-924	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	>100 μM Compound: 2, PR-924	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]
RPMI-8226	IC₅₀	>100 μM Compound: 2, PR-924	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	0.025 μM Compound: 2, PR-924	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	2.9 μM Compound: 2, PR-924	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	3.5 μM Compound: 2, PR-924	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]

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.

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.

Chemical Information

CAS. Nr. 1416709-79-9
Appearance Solid
Molecular Weight 618.72
Formel C₃₇H₃₈N₄O₅
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6162 mL

8.0812 mL

16.1624 mL

5 mM

0.3232 mL

1.6162 mL

3.2325 mL

10 mM

0.1616 mL

0.8081 mL

1.6162 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

PR-924

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PR-924

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PR-924 Related Classifications

HY-123587 Related Classifications