GNE-987 Inhibitor

Name: GNE-987 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5753210
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5753210

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 4.4nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03nM for… More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

GNE-987, Inhibitor

Full Product Name

GNE-987

Product Gene Name

GNE-987, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

1096.31

Solubility

<1mg/ml refers to the product slightly soluble or insoluble

Formula

C56H67F2N9O8S2

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

Target & IC50

BRD4(BD1): ic50 4.7nM
BRD4 BD2: ic50 4.4nM
VHL

In Vitro

GNE-987 (0.1-10nM; 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 0.03nM, respectively, and inhibits MYC expression with an IC50 of 0.03nM.

Product Categories/Family for GNE-987, inhibitor

Chromatin/Epigenetic; Epigenetic Reader Domain

Product References and Citations for GNE-987, inhibitor

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

Other Notes

Small volumes of GNE-987, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for GNE-987 purchase

MBS5753210 is an inhibitor targeting GNE-987.