VZ185
Based on 2 publication(s) in Google Scholar
VZ185 is a BRD9 and BRD7 PROTAC degrader, with DC50 values of 1.76 nM and 4.5 nM, respectively, in RI-1 cells; and DC50 values of 4 nM and 34 nM, respectively, in HEK293 cells. VZ185 hijacks the CRL2VHL E3 ubiquitin ligase complex to induce ubiquitination and subsequent proteasomal degradation of BRD9 and BRD7. VZ185 can be used in research related to acute myeloid eosinophilic leukemia and malignant rhabdoid tumors.
(Pink: BRD9 and BRD7 ligand (HY-111905A); Blue: VHL ligand (HY-125905); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
The VZ185 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Pureza: 99.95%
- No. CAS: 2306193-61-1
- Fòrmula: C53H67FN8O8S
- Peso molecular:995.21
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) VZ185
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Actividad biológica
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BRD9 1.76 nM (DC50) |
BRD7 4.5 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
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| A204 | IC50 |
0.03981 μM
Compound: 51; VZ185
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Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
Antiproliferative activity against human A204 cells assessed as inhibition of cell growth incubated for 7 days by CellTiterGlo assay
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[PMID: 30540463] |
VZ185 (0.001-1 μM; 24 h) potently, rapidly and concentration-dependently degrades endogenously labeled BRD9 and BRD7 in HEK293 cells, with a preference for BRD9[1].
VZ185 (0.0001-100 μM; 7 days) potently reduces the viability of BRD9-sensitive EOL-1 and A-204 cancer cell lines, with IC50 values of 3.389 nM and 39.81 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EOL-1 (acute myeloid eosinophilic leukemia) cells, A-204 (malignant rhabdoid tumor) cells
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Concentration:0.0001, 0.01, 1, and 100 μM
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Incubation Time:7 day
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Result:Exhibited cytotoxicity to both cell lines, with an EC50 of 3 nM in EOL-1 cells and 40 nM in A-204 cells.
Chemical Information
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No. CAS 2306193-61-1
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Appearance Solid
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Peso molecular 995.21
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Fòrmula C53H67FN8O8S
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3OCCCCCN5CCN(CC6=C(OC)C=C(C(C7=CC=NC=C87)=CN(C)C8=O)C=C6OC)CC5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Solvente y solubilidad
DMSO : 200 mg/mL (200.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. Journal of medicinal chemistry. 2019 Jan 24;62(2):699-726. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.0048 mL | 5.0241 mL | 10.0481 mL | 25.1203 mL |
| 5 mM | 0.2010 mL | 1.0048 mL | 2.0096 mL | 5.0241 mL | |
| 10 mM | 0.1005 mL | 0.5024 mL | 1.0048 mL | 2.5120 mL | |
| 15 mM | 0.0670 mL | 0.3349 mL | 0.6699 mL | 1.6747 mL | |
| 20 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2560 mL | |
| 25 mM | 0.0402 mL | 0.2010 mL | 0.4019 mL | 1.0048 mL | |
| 30 mM | 0.0335 mL | 0.1675 mL | 0.3349 mL | 0.8373 mL | |
| 40 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6280 mL | |
| 50 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5024 mL | |
| 60 mM | 0.0167 mL | 0.0837 mL | 0.1675 mL | 0.4187 mL | |
| 80 mM | 0.0126 mL | 0.0628 mL | 0.1256 mL | 0.3140 mL | |
| 100 mM | 0.0100 mL | 0.0502 mL | 0.1005 mL | 0.2512 mL |
VZ185 Related Classifications
HY-114322 Related Classifications
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