PI-1840 [Proteasome Inhibitor]

CHF 30.00
In stock
AG-CR1-3675-M0011 mgCHF 30.00
AG-CR1-3675-M0055 mgCHF 80.00
AG-CR1-3675-M02525 mgCHF 270.00
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Product Details
Synonyms N-(1-Methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-acetamide
Product Type Chemical
Properties
Formula

C22H26N4O3

MW 394.5
CAS 1401223-22-0
Purity Chemicals ≥95% (HPLC)
Appearance White solid.
Solubility Soluble in DMSO (30mg/ml) or ethanol (20mg/ml). Poorly soluble in aqueous solutions.
Identity Determined by 1H-NMR.
Other Product Data

Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. Stock solutions are stable for at least 1 month when stored at -20°C.

InChi Key ZVVXAODXPVWGMF-UHFFFAOYSA-N
Smiles CCCC1=CC=C(OCC(N(CC2=NC(C3=CC=CN=C3)=NO2)C(C)C)=O)C=C1
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Highly potent, selective and rapidly reversible non-covalent proteasome inhibitor.
  • Targets the chymotrypsin-like β5-subunit of the constitutive 20S proteasome (IC50=27nM), with minimal cross-reactivity on the trypsin-like (β2) and caspase-like/postglutamyl-peptide-hydrolysis-like (β1) proteolytic activity (IC50= >100μM, for both). Exhibited over 100-fold selectivity for the constitutive 20S proteasome over the immunoproteasome.
  • Anticancer compound.
  • In vitro, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability and induces apoptosis in intact cancer cells.
  • Shown to inhibit tumor growth in mice of MDA-MB-231 breast tumors.
Product References
  1. Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors: S. Ozcan, et al.; J. Med. Chem. 56, 3783 (2013)
  2. Discovery of PI-1840, a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity: A. Kazi, et al.; J. Biol. Chem. 289, 11906 (2014)
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