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GNE-987

Catalog No. BP13868  

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).

This Product is For Research Use Only.
GNE-987
Pack Size Availability Price/USD Quantity
1 mg Inquiry $ 556
2 mg Inquiry $ 945
4 mg Inquiry $ 1600
10 mg Inquiry $ 3040
20 mg Inquiry $ 4833
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Product 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.
Chemical Formula C56H67F2N9O8S2
Molecular Weight 1096.31
Storage Powder: -20°C for 2 years
In solvent: -80°C for 1 year

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