GNE-987
Based on 1 publication(s) in Google Scholar
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer.
(Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-123109); Black: linker (HY-W013253)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 2417371-71-0
- Fòrmula: C56H67F2N9O8S2
- Peso molecular:1096.31
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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) GNE-987
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Flow Cytometry
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WB
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Apoptosis Analysis
Ver todos los productos específicos de isoformas PROTACs
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Actividad biológica
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VHL |
BRD4 (BD1) 4.7 nM (IC50) |
BRD4 (BD2) 4.4 nM (IC50) |
GNE-987 inhibits EOL-1 and HL-60 cell viability with IC50s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC50 of 0.03 nM[1].
GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins[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 cells
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Concentration:0.1, 1, 10 nM
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Incubation Time:5 hours
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Result:Degraded the BRD2 and BRD3 BET family proteins.
Chemical Information
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No. CAS 2417371-71-0
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Appearance Solid
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Peso molecular 1096.31
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Fòrmula C56H67F2N9O8S2
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Color White to off-white
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SMILES
O=C([C@H](C[C@@H](O)C1)N1C([C@@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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BMC Cancer
The BET PROTAC inhibitor GNE-987 displays anti-tumor effects by targeting super-enhancers regulated gene in osteosarcoma. [Abstract]2024 Aug 1;24(1):928. PMID: 39090568
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0.625-160 nM; 48 h) inhibited cell viability in U2OS, HOS, MG-63, 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0, 2.5, 5, 10 nM; 7–12 days) inhibited the colony formation of OS cells in a dose-dependent manner in U2OS, HOS, MG-63, 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (10; 20 nM; 24 h) resulted in G2/M arrest of OS cell lines compared to control groups using Modfit analysis in U2OS, HOS, MG-63, 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0, 2.5, 5, 10 nM; 24 h) downregulated the protein expression of Cyclin B1 in a dose-dependent manner in U2OS, HOS, MG-63, 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (10, 20 nM; 24 h) induced apoptosis in a dose-dependent manner in U2OS, HOS, MG-63, 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (10, 20 nM; 24 h) degraded BET and RUNX2 protein expression in U2OS, HOS, MG-63, and 143B cells.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0.2 mg/kg; ip; every two days for 18 days) showed that tumor mass and volume were significantly reduced in BALB/c nude mice with HOS cells were subcutaneously injected.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0.2 mg/kg; ip; every two days for 18 days) showed no significant toxic response in the internal organs in BALB/c nude mice with HOS cells that were subcutaneously injected.
GNE-987 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]
GNE-987 (0.2 mg/kg; ip; every two days for 18 days) significantly reduced the expression levels of BRD4 and Ki-67 in the tumors.
Solvente y solubilidad
DMSO : 100 mg/mL (91.22 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 (stored under nitrogen). 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 (stored under nitrogen). 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (274 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
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 (stored under nitrogen). 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 | 0.9122 mL | 4.5608 mL | 9.1215 mL | 22.8038 mL |
| 5 mM | 0.1824 mL | 0.9122 mL | 1.8243 mL | 4.5608 mL | |
| 10 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2804 mL | |
| 15 mM | 0.0608 mL | 0.3041 mL | 0.6081 mL | 1.5203 mL | |
| 20 mM | 0.0456 mL | 0.2280 mL | 0.4561 mL | 1.1402 mL | |
| 25 mM | 0.0365 mL | 0.1824 mL | 0.3649 mL | 0.9122 mL | |
| 30 mM | 0.0304 mL | 0.1520 mL | 0.3041 mL | 0.7601 mL | |
| 40 mM | 0.0228 mL | 0.1140 mL | 0.2280 mL | 0.5701 mL | |
| 50 mM | 0.0182 mL | 0.0912 mL | 0.1824 mL | 0.4561 mL | |
| 60 mM | 0.0152 mL | 0.0760 mL | 0.1520 mL | 0.3801 mL | |
| 80 mM | 0.0114 mL | 0.0570 mL | 0.1140 mL | 0.2850 mL |
GNE-987 Related Classifications
HY-129937A Related Classifications
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