GNE-0011 | BRD4 degrader | Probechem Biochemicals

Chemical Structure : GNE-0011

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GNE-0011 (GNE 0011)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	475.61
分子式	C26H29N5O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	tert-butyl (S)-2-(4-(4-(3-aminoprop-1-yn-1-yl)phenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate

参考文献

1. Blake, R. A. Abstract 4452: GNE-0011, a novel monovalent BRD4 degrader. Cancer Res. 79, 4452 (2019).

GNE-0011 (GNE 0011)

生物&药学活性

物理化学性质&存储条件

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GNE-0011 (GNE 0011)

生物&药学活性

物理化学性质&存储条件

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