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Chemical Structure : GNE-0011
Catalog No.: PC-21848Not For Human Use, Lab Use Only.
GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
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GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
GNE-0011 shows low nanomolar inhibition of c-Myc in cells (IC50 = 2 nM).
GNE-0011 shows anticance efficacy in a mouse xenograft model (EOL-1) at low doses (3 mg/kg QD IP).
The mechanism by which this monovalent pan-BET binder leads to selective BRD4 degradation is not fully understood.
| M.Wt | 475.61 | |
| Formula | C26H29N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Blake, R. A. Abstract 4452: GNE-0011, a novel monovalent BRD4 degrader. Cancer Res. 79, 4452 (2019).
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