Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | Inquiry | $ 494.00 | |
5 mg | Inquiry | $ 1,120.00 | |
10 mg | Inquiry | $ 1,780.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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GNE-987 2417371-71-0 Chromatin/Epigenetic Epigenetic Reader Domain GNE987 GNE 987 inhibitor inhibit