VZ 185

Catalog #: 6936 Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
6936/5

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%

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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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) and BRD7 antibody validated for Western Blot also available: Catalog # NBP1-28727.

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

Technical Data

E3 ligase

VHL

DC₅₀ / D_max

4.5 nM / 95% (BRD7), 1.79 nM / 95% (BRD9) - Degradation in RI-1 cells after 8 h treatment

Selectivity confirmed by global proteomics

Yes

M.Wt:

995.23

Formula:

C₅₃H₆₇FN₈O₈S

Solubility:

Soluble to 100 mM in DMSO

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

2306193-61-1

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.

Background References

Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel-Lindau (VHL) based dual degrader probe of BRD9 and BRD7.
Zoppi et al.
J.Med.Chem., 2019;62:699

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