Art. -Nr.: HY-129937A

GNE-987

1 Cited Publications

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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)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.98%
CAS. Nr.: 2417371-71-0
Formel: C₅₆H₆₇F₂N₉O₈S₂
Molecular Weight:1096.31

Speicherung:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

GNE-987 Chemical Structure

CAS. Nr.: 2417371-71-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Publications Citing Use of MedChemExpress (MCE) GNE-987

BMC Cancer. 2024 Aug 1;24(1):928. [Abstract]

Customer Validation & Images

Cell Proliferation/Viability AssayCell Migration/Invasion AssayFlow CytometryWBApoptosis AnalysisIn Vivo Efficacy StudyHistological Imaging/StainingIHC

Cell Proliferation/Viability Assay
Cell Migration/Invasion Assay
Flow Cytometry
WB
Apoptosis Analysis
WB
In Vivo Efficacy Study
Histological Imaging/Staining
IHC

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-123109); Black: linker (HY-W013253)).

IC₅₀ & Target^[1]

VHL

BRD4 (BD1)

4.7 nM (IC₅₀)

BRD4 (BD2)

4.4 nM (IC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

EOL-1 cells
Concentration:

0.1, 1, 10 nM
Incubation Time:

5 hours
Result:

Degraded the BRD2 and BRD3 BET family proteins.

Chemical Information

CAS. Nr. 2417371-71-0
Appearance Solid
Molecular Weight 1096.31
Formel C₅₆H₆₇F₂N₉O₈S₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (1)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayFlow CytometryWBApoptosis AnalysisIn Vivo Efficacy StudyHistological Imaging/StainingIHC

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Journal Impact Factor

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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9122 mL

4.5608 mL

9.1215 mL

5 mM

0.1824 mL

0.9122 mL

1.8243 mL

10 mM

0.0912 mL

0.4561 mL

0.9122 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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

Keywords

GNE-987

1 Cited Publications

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GNE-987

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) GNE-987

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-987 Related Classifications

HY-129937A Related Classifications