PI-1840

• CAT Number: I001529
• CAS Number: 1401223-22-0
• Molecular Formula: C22H26N4O3
• Molecular Weight: 394.47
• Purity: ≥95%
• Synonyms: N-isopropyl-2-(4-propylphenoxy)-N-((3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)methyl)acetamide
• Target: Proteasome
• Solubility: 10 mM in DMSO
• Storage: Desiccate at -20°C
• IC50: 27 nM(CT-L activities of the proteasome)
• IUPAC Name: N-propan-2-yl-2-(4-propylphenoxy)-N-[(3-pyridin-3-yl-1,2,4-oxadiazol-5-yl)methyl]acetamide
• InChI: InChI=1S/C22H26N4O3/c1-4-6-17-8-10-19(11-9-17)28-15-21(27)26(16(2)3)14-20-24-22(25-29-20)18-7-5-12-23-13-18/h5,7-13,16H,4,6,14-15H2,1-3H3
• InChIKey: ZVVXAODXPVWGMF-UHFFFAOYSA-N
• SMILES: CCCC1=CC=C(C=C1)OCC(=O)N(CC2=NC(=NO2)C3=CN=CC=C3)C(C)C

PI-1840（Cat No.:I001529）is a reversible and selective inhibitor that specifically targets the chymotrypsin-like (CT-L) proteasomal activity. It demonstrates potent inhibition against CT-L with an IC50 value of 27nM. However, it does not significantly affect the proteolytic activity of the other two major proteasome subunits, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). This selectivity allows for specific modulation of CT-L activity without interfering with the function of other proteasomal subunits. PI-1840 holds potential as a research tool for studying the role of CT-L proteasomal activity in various biological processes.

Reference

[1]. Kazi A, et al. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. J Biol Chem. 2014 Apr 25;289(17):11906-15.