bs-75558C

DATASHEET

Formulation Solid

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

Product Information:

CAS Number: 868540-17-4

Molecular formula: C40H57N5O7

Molecular weight: 719.9

Purity: >98% (HPLC)

Appearance: White solid.

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

InChiKey: BLMPQMFVWMYDKT-NZTKNTHTSA-N

SMILES: O=C([C@]1(C)OC1)[C@H](CC(C)C)NC([C@H](CC2=CC=CC=C2)NC([C@H](CC(C)C)NC([C@H](CCC3=CC=CC=C3)NC(CN4CCOCC4)=O)=O)=O)=O

Description:

Potent and irreversible second-generation peptide epoxyketone class proteasome inhibitor. Synthetic analog of the microbial product epoxomicin (Prod. No. bs-75199C). Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=5.2nM) and the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=14nM), with minimal cross-reactivity to other proteases. Displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome compared to bortezomib (Prod. No. bs-75509C). Anticancer compound effective against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma and various solid tumors (IC50s=2.4-20nM).