VZ 185

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VZ 185 | CAS No. 2306193-61-1 | Active Degraders
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Description: Potent and selective BRD7/9 Degrader (PROTAC®)

Chemical Name: (2S,4R)-N-(2-((5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide

Purity: ≥98%

Product Details
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Biological Activity

VZ 185 is a potent and selective VHL-based dual Degrader (PROTAC®) of BRD7/9 (DC50 values are 4 and 34 nM for BRD7 and BRD9, respectively). Exhibits selectivity for BRD7/9 degradation over other bromodomain-containing proteins and other BAF/PBAF subunits. Displays cytotoxicity towards EOL-1 and A-204 cancer cell lines.

Negative control cis VZ 185 (Cat. No. 6939) also available.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data

E3 ligase
DC50 / Dmax
4.5 nM / 95% (BRD7), 1.79 nM / 95% (BRD9) - Degradation in RI-1 cells after 8 h treatment
Selectivity confirmed by global proteomics
Soluble to 100 mM in DMSO
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under licence from the University of Dundee.

Product Datasheets

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