PI-1840

SKU: orb1300327

Description

PI-1840 is a potent, reversible, and selective inhibitor of the proteasome's chymotrypsin-like (CT-L) activity (IC50 = 27 nM), exhibiting minimal effect on trypsin-like and postglutamyl-peptide-hydrolysis-like activities. This compound is a valuable research tool for studying proteasome function in cellular models and has been utilized in investigations of cancer and neurodegenerative disease pathways.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 1401223-22-0
• MW: 394.47
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₂₆N₄O₃
• SMILES: CCCc1ccc(OCC(=O)N(Cc2nc(no2)-c2cccnc2)C(C)C)cc1
• Target: Autophagy,Caspase,Bcl-2 Family,PARP,Proteasome,NF-κB,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.07 mM);Ethanol:31 mg/mL (78.59 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:72 mg/mL (182.52 mM)

Bioactivity

• Target IC50:
  Chymotrypsin-like proteasome:27 nM
• In Vivo:
  PI-1840 (150 mg/kg i.p.) inhibits the tumor growth in mice of MDA-MB-231 breast tumors.
• In Vitro:
  PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human MDA-MB-468 cells. In intact cancer cells, PI-1840 inhibits CT-L activity, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis.
• Cell Research:
  Cells are plated in 96-well plates in 100 μL medium and allowed to attach overnight. Cells are then incubated for 120 h with varying concentrations of inhibitors. Media is aspirated and replaced with 100 μL complete media containing 1 mg/ml MTT and incubated for three hours at 37 °C in 5% CO2 humidified incubator. Media is then aspirated and DMSO is added. Cells are incubated for 10 min at room temperature while shaking, and the absorbance is determined at 540 nm using a μQuant spectrophotometric plate reader. The IC50 values are determined using equation under CT-L, T-L, PGPH-L proteolytic activity assays.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cell proliferation, cell cycle, Chymotrypsin-like proteasome, Bcl-2 Family, Caspase, Autophagy, anticancer, Apoptosis, Inhibitor, inhibit, MG-63 cells, PARP, Nuclear factor-kappaB, Nuclear factor-κB, NF-κB, poly ADP ribose polymerase, PI1840, PI-1840, PI 1840, Proteasome, proteasome substrates, U2-OS cells

Compound Identifiers

PubChem CID

56945245