bs-75564C

DATASHEET

Formulation Solid

Storage: Stable for 2 years after receipt when stored at -20°C.

Product Information:

CAS Number: 1401223-22-0

Molecular formula: C22H26N4O3

Molecular weight: 394.5

Purity: >95% (HPLC)

Appearance: White solid.

Solubility: Soluble in DMSO (30mg/ml) or ethanol (20mg/ml). Poorly soluble in aqueous solutions.

InChiKey: ZVVXAODXPVWGMF-UHFFFAOYSA-N

SMILES: CCCC1=CC=C(OCC(N(CC2=NC(C3=CC=CN=C3)=NO2)C(C)C)=O)C=C1

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.