1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. GNE-987

GNE-987 

Cat. No.: HY-129937A
Handling Instructions

GNE-987 is a highly active chimeric BET degrader. 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).

For research use only. We do not sell to patients.

GNE-987 Chemical Structure

GNE-987 Chemical Structure

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Description

GNE-987 is a highly active chimeric BET degrader. 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)[1].

IC50 & Target[1]

BRD4 (BD1)

4.7 nM (IC50)

BRD4 (BD2)

4.4 nM (IC50)

VHL

 

In Vitro

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[1].
GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins[1].

Western Blot Analysis[1]

Cell Line: EOL-1 cells
Concentration: 0.1, 1, 10 nM
Incubation Time: 5 hours
Result: Degraded the BRD2 and BRD3 BET family proteins.
Molecular Weight

1096.31

Formula

C₅₆H₆₇F₂N₉O₈S₂

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GNE-987GNE987GNE 987PROTACEpigenetic Reader DomainProteolysis-targeting chimerachimericBETdegraderEOL-1 cellsHL-60 cellsdegradation-inactiveMYCInhibitorinhibitorinhibit

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Product name:
GNE-987
Cat. No.:
HY-129937A
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