| Chemical Properties | Back Directory | [Boiling point ]
1116.1±65.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 200 mg/mL (200.96 mM; Need ultrasonic) | [form ]
Solid | [pka]
13.79±0.20(Predicted) | [color ]
White to off-white | [InChIKey]
ZAGCLFXBHOXXEN-JPTLTNPLSA-N | [SMILES]
FC8(CC8)C(=O)N[C@@H](C(C)(C)C)C(=O)N1[C@@H](C[C@H](C1)O)C(=O)NCc2c(cc(cc2)c7[s]cnc7C)OCCCCCN3CCN(CC3)Cc4c(cc(cc4OC)c5c6c([c]([n](c5)C)=O)cncc6)OC |
| Hazard Information | Back Directory | [Uses]
VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively[1]. | [Biological Activity]
VZ185 is a potent and selective bromodomain proteins BRD7 and BRD9 degrader th at targets BRD7/9 for von Hippel-Lindau (VHL) ubiquitin ligase complex-mediated degradation. VZ185 effectively induces cellular BRD7/9 degradation (by 90% BRD7 & 86% BRD9 in 4 h in HeLa cellsby 84% BRD7 in 2 h in RI-1 cells; BRD7/9 IC50 = 4.5/1.76 nM in 8 h in RI-1 cells) and exerts potent cytotoxicity in BRD9-dependent cancer cultures (IC50 = 3.389 nM/EOL-1 & 39.81 nM/A-204 post 7-day treatment). | [IC 50]
BRD7: 4.5 nM (DC50); BRD9: 1.8 nM (DC50) | [storage]
Store at -20°C | [References]
[1] Zoppi V, et al. 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 Jan 24;62(2):699-726. DOI:10.1021/acs.jmedchem.8b01413 |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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