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VZ185

Chemical Structure : VZ185

CAS No.: 2306193-61-1

VZ185 (VZ-185;VZ 185)

Catalog No.: PC-35882Not For Human Use, Lab Use Only.

VZ185 (VZ-185) is a potent, fast and selective, VHL-based dual degrader probe (PROTAC) of BRD9 and BRD7 with DC50 of 1.8 and 4.5 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VZ185 (VZ-185) is a potent, fast and selective, VHL-based dual degrader probe (PROTAC) of BRD9 and BRD7 with DC50 of 1.8 and 4.5 nM, respectively.
VZ185 induces strong and rapid degradation of of BRD9, BRD7 in a time- and dose-dependent manner after treatment of RI-1 cells, also shows a DC50 between 2-8 nM for BRD9 in a panel of other human cancer cell lines (EOL-1, A-204).

Physicochemical Properties

M.Wt 995.225
Formula C53H67FN8O8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Zoppi V, et al. J Med Chem. 2018 Dec 12. doi: 10.1021/acs.jmedchem.8b01413.

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