Formulation: A solid
Formal Name: N-(1-methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-acetamide
Purity: ≥98%
Formula Markup: C22H26N4O3
Formula Weight: 394,5
Shelf life (days): 1460
CAS Number: 1401223-22-0
Notes: PI-1840 is an inhibitor of chymotrypsin-like (CTL) proteasome activity (IC50 = 27 nM).{66509} It is selective for the CTL activity over the trypsin-like (TL) and peptidylglutamyl peptide hydrolyzing (PGPH) activities (IC50s = >100 µM for both), as well as for the 20S constitutive proteasome over the immunoproteasome (IC50s = 18 and 2,170 nM, respectively). PI-1840 decreases the viability of a panel of cancer cell lines (IC50s = 2.2-45.2 µM). It induces cell cycle arrest at the G2/M phase, apoptosis, and autophagy, as well as inhibits migration and invasion, in U2OS and MG-63 osteosarcoma cells when used at concentrations of 40 and 60 µM, respectively.{66510} PI-1840 (150 mg/kg) decreases tumor volume in an MDA-MB-231 breast cancer mouse xenograft model.{66509}
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