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GNE-987

Cat. No.: IBDI-434896

GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). 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 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).

Size (Solid):

Product Details

Target PROTACs | Epigenetic Reader Domain
Molecular Weight 1096.31
Appearance Solid
SMILES O=C([[email protected]](C[[email protected]@H](O)C1)N1C([[email protected]@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7
Purity 99.91%

Storage & Handling

Shipping Room temperature in continental US. May vary elsewhere.
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Regulatory Status This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use.
! For research use only, not intended for any clinical use.