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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

😃Good

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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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline /PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Stock solution preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(stock solution concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline /PBS/ddH₂O TargetMol | reagent

mix well and clarify

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