AdipoGen Life Sciences

PI-1840 [Proteasome Inhibitor]

Product Code:
 
AG-CR1-3675
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Shipping:
 
Ambient
Storage:
 
-20°C
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Chemical Structure
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Chemical Structure

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Further Information

Alternate Names/Synonyms:
N-(1-Methylethyl)-2-(4-propylphenoxy)-N-[[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]methyl]-acetamide
Appearance:
White solid.
CAS:
1401223-22-0
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Keep cool and dry.
Hazards:
H315, H319, H335
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
Long Description:
Chemical. CAS: 1401223-22-0. Formula: C22H26N4O3. MW: 394.5. Synthetic. Highly potent, selective and rapidly reversible non-covalent proteasome inhibitor. Targets the chymotrypsin-like beta5-subunit of the constitutive 20S proteasome (IC50=27nM), with minimal crossreactivity on the trypsin-like (beta2) and caspase-like/postglutamyl-peptide-hydrolysis-like (beta1) 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 IkappaB-alpha, 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.
MDL:
MFCD28142700
Molecular Formula:
C22H26N4O3
Molecular Weight:
394.5
Other 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.
Package Type:
Plastic Vial
Precautions:
P280, P302, P352, P304, P340, P305, P351, P338, P332, P337, P313, P405
Product Description:
Highly potent, selective and rapidly reversible non-covalent proteasome inhibitor. Targets the chymotrypsin-like beta5-subunit of the constitutive 20S proteasome (IC50=27nM), with minimal cross-reactivity on the trypsin-like (beta2) and caspase-like/postglutamyl-peptide-hydrolysis-like (beta1) 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 IkappaB-alpha, 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.
Purity:
>95% (HPLC)
Signal word:
Warning
SMILES:
CCCC1=CC=C(OCC(N(CC2=NC(C3=CC=CN=C3)=NO2)C(C)C)=O)C=C1
Solubility Chemicals:
Soluble in DMSO (30mg/ml) or ethanol (20mg/ml). Poorly soluble in aqueous solutions.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

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)