AdipoGen Life Sciences

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

Description

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

Oxadiazole-isopropylamides as potent and noncovalent proteasome inhibitors: S. Ozcan, et al.; J. Med. Chem. 56, 3783 (2013)
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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