NSC 687852 - 10mM in DMSO, high purity , CAS No.1009817-63-3

Item Number

N420305

• Synonyms: b-AP15 | 1009817-63-3 | (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one | NSC687852 | NSC 687852 | 4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-1-(1-oxo-2-propen-1-yl)-, (3E,5E)- | NSC-687852 | (3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-(prop-2-en
• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: In Vitro：Purified 19S proteasomes (5 nM) are treated with indicated concentrations of b-AP15 and DUB activity is determined by detectionof Ub-AMC cleavage. The IC50 value (2.1±0.411 μM) is determined from log concentration curves in Graph Pad Prism using
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

A cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo.