PI-1840 [Proteasome Inhibitor]
30 CHF CHF 30.00
AG-CR1-3675-M0011 mgCHF 30.00
AG-CR1-3675-M0055 mgCHF 80.00
AG-CR1-3675-M02525 mgCHF 270.00
|Purity Chemicals||≥95% (HPLC)|
|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.
|Shipping and Handling|
|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.|
|Product Specification Sheet|
- 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.
- 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)