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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $494 | Backorder | |
5 mg | $1,120 | Backorder | |
10 mg | $1,780 | Backorder |
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 |
Targets&IC50 | VHL:, BRD4 BD1:4.7 nM, BRD4 BD2:4.4 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 |
Relative Density. | 1.40 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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