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GNE-987

Name: GNE-987
Brand: TargetMol
SKU: T11441
Rating: 4.5 (1 reviews)

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Catalog No. T11441Cas No. 2417371-71-0

Alias GNE987, GNE 987

GNE-987 is a highly active chimeric BET degrader that binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low-nanomolar affinity and induces exceptionally potent BRD4 degradation in cells, achieving picomolar DC50 values in EOL-1 acute myeloid leukemia cells, thereby serving as a powerful chemical biology tool for dissecting BET-dependent transcriptional regulation.

GNE-987

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Catalog No. T11441Alias GNE987, GNE 987Cas No. 2417371-71-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$494	Inquiry	Inquiry
5 mg	$1,120	Inquiry	Inquiry
10 mg	$1,780	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	GNE-987 is a highly active chimeric BET degrader that binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low-nanomolar affinity and induces exceptionally potent BRD4 degradation in cells, achieving picomolar DC50 values in EOL-1 acute myeloid leukemia cells, thereby serving as a powerful chemical biology tool for dissecting BET-dependent transcriptional regulation.
Targets&IC50	BRD4 BD2:4.4 nM, VHL:, BRD4 BD1:4.7 nM
In vitro	GNE-987 shows IC₅₀ values of 4.7 nM for the BD1 domain and 4.4 nM for the BD2 domain. In EOL-1 cells, the molecule facilitates the proteasomal degradation of BRD2 and BRD3 within 5 hours at concentrations between 0.1-10 nM. This process results in the suppression of the oncogenic transcription factor MYC, inhibiting its expression with an IC₅₀ of 0.03 nM [1].
Synonyms	GNE987, GNE 987

Chemical Properties

Molecular Weight	1096.31
Formula	C₅₆H₆₇F₂N₉O₈S₂
Cas No.	2417371-71-0
Smiles	O=C1C2=C3C(C=4C(N(CC3=CN2)C5=C(F)C=C(F)C=N5)=CC(C(NCCCCCCCCCCC(N[C@H](C(=O)N6[C@H](C(NCC7=CC=C(C=C7)C8=C(C)N=CS8)=O)C[C@@H](O)C6)[C@@](C)(C)C)=O)=O)=C(CS(C)(=O)=O)C4)=CN1C
Relative Density.	1.40 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (72.97 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.9122 mL	4.5608 mL	9.1215 mL	45.6075 mL
5 mM	0.1824 mL	0.9122 mL	1.8243 mL	9.1215 mL
10 mM	0.0912 mL	0.4561 mL	0.9122 mL	4.5608 mL
20 mM	0.0456 mL	0.2280 mL	0.4561 mL	2.2804 mL
50 mM	0.0182 mL	0.0912 mL	0.1824 mL	0.9122 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc