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

PR-924 

Cat. No.: HY-123587
Handling Instructions

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.

For research use only. We do not sell to patients.

PR-924 Chemical Structure

PR-924 Chemical Structure

CAS No. : 1416709-79-9

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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].

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].

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.

1416709-79-9

SMILES

O=C(N[[email protected]@H](CC1=CC=CC=C1)C([[email protected]]2(CO2)C)=O)[[email protected]@H](NC([[email protected]@H](C)NC(C(CC3=CC=CC=C43)=C4C)=O)=O)CC5=CNC6=CC=CC=C56

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PR-924PR924PR 924ProteasomeApoptosisLMP-7tripeptideepoxyketonecovalentlyN-terminalthreonineshIL-6Rβ5imitochondriaantitumorapoptosisInhibitorinhibitorinhibit

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