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PR-924

Chemical Structure : PR-924

CAS No.: 1416709-79-9

PR-924 (IPSI;PR 924;PR924)

Catalog No.: PC-60963Not For Human Use, Lab Use Only.

A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM); shows weak activity toward LMP2 and no detectable activity toward β1, β2, or MECL1.

Physicochemical Properties

M.Wt 618.734
Formula C37H38N4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((R)-1-(((S)-3-(1H-indol-3-yl)-1-(((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)amino)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)-3-methyl-1H-indene-2-carboxamide

References

1. Parlati F, et al. Blood. 2009 Oct 15;114(16):3439-47.

2. de Bruin G, et al. J Med Chem. 2014 Jul 24;57(14):6197-209.

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