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

GNE-987 is a highly active chimeric BET degrader. 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 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line).

GNE-987

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Catalog No. T11441Cas 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. 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 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line).
Targets&IC50	VHL:, BRD4 BD2:4.4 nM, BRD4 BD1:4.7 nM
In vitro	GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins.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.

Chemical Properties

Molecular Weight	1096.31
Formula	C₅₆H₆₇F₂N₉O₈S₂
Cas No.	2417371-71-0
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
Relative Density.	1.40 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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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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