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VZ185

2D structure
Target BRD7  BRD9 
Mode of action PROTAC degrader
Control cisVZ185
Recommended cellular usage concentration 300 nM
In vivo use No
Donated by Dundee University


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Isothermal titration calorimetry (ITC) (KD = 26 ± 9 nM binary (VHL:VZ185), 27 ± 3 nM ternary (VHL:VZ185:BRD9-BD), 5.1 ± 0.6 nM binary (VZ185:BRD9-BD) (n ≥ 2); Fluorescence polarization (FP) (KD = 35 ± 5 nM binary (VHL:VZ185), 35 ± 6 nM ternary (VHL:VZ185:BRD9-BD) (n>2)),
Selectivity within target family: > 30-fold Highly selective
Selectivity outside target family Highly selective: No off-targets detected in cellular proteosome
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: BRD7: DC50 = 4.5 nM; BRD9: DC50 = 1.76 nM (degradation of BRD7/9 in RI-1 cells after 8 h)
Live cell degradation HiBiT-BRD7: DC50 = 34.5 nM, HiBiT-BRD9: DC50 = 4.0 nM
Cytotoxic in cancer cell lines: Cell viability (CellTiterGlo): EC50 = 3.4 nM (EOL-1), EC50 = 39.8 nM (A-402)
Control compound (100 times less potent than the probe) cisVZ185: no degradation of BRD7/9 observed