VZ 185

Name: VZ 185
Brand: Tocris Bioscience
SKU: 6936

Tocris Bioscience, part of Bio-Techne | Catalog # 6936

Citations (1)

COA / SDS

Potent and selective BRD7/9 Degrader (PROTAC®)

Key Product Details

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% (HPLC)
Molecular Weight:	995.23

View Full Technical Details for VZ 185

Technical Data
Citations

Biological Activity for VZ 185

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.

Licensing Information

Sold under licence from the University of Dundee.

Technical Data for VZ 185

M. Wt	995.23
Formula	C₅₃H₆₇FN₈O₈S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2306193-61-1
PubChem ID	138454768
InChi Key	ZAGCLFXBHOXXEN-JPTLTNPLSA-N
Smiles	CN(C(C1=C2C=CN=C1)=O)C=C2C3=CC(OC)=C(C(OC)=C3)CN4CCN(CC4)CCCCCOC5=CC(C6=C(N=CS6)C)=CC=C5CNC([C@@H]7C[C@H](CN7C([C@H](C(C)(C)C)NC(C8(CC8)F)=O)=O)O)=O
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

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.

Solubility for VZ 185

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	99.52	100

Preparing Stock Solutions for VZ 185

The following data is based on the product molecular weight 995.23.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.00 mL	5.02 mL	10.05 mL
5 mM	0.20 mL	1.00 mL	2.01 mL
10 mM	0.10 mL	0.50 mL	1.00 mL
50 mM	0.02 mL	0.10 mL	0.20 mL

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References for VZ 185

References are publications that support the biological activity of the product.

Riching Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation. Curr.Res.Chem.Biol.
Zoppi 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. J.Med.Chem. 2019 PMID: 30540463