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GNE-987

Catalog No. T11441   CAS 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).

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GNE-987 Chemical Structure
GNE-987, CAS 2417371-71-0
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1 mg Inquiry $ 494.00
5 mg Inquiry $ 1,120.00
10 mg Inquiry $ 1,780.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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 BRD4 BD2:4.4 nM, VHL:, 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.
Molecular Weight 1096.31
Formula C56H67F2N9O8S2
CAS No. 2417371-71-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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

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Keywords

GNE-987 2417371-71-0 Chromatin/Epigenetic Epigenetic Reader Domain GNE987 GNE 987 inhibitor inhibit

 

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