GNE-987 |
| Katalog-Nr.GC60883 |
GNE-987 ist ein PROTAC, das durch Liganden fÜr von Hippel-Lindau und BRD4 verbunden ist. GNE-987 zeigt pikomolare BRD4-ZellabbauaktivitÄt (DC50 = 0,03 nM fÜr EOL-1 AML-Zelllinie). GNE-987 bindet Äquipotent an die BD1- und BD2-BromdomÄnen von BRD4 mit niedrigen nanomolaren AffinitÄten (IC50 = 4,7 bzw. 4,4 nM). GNE-987 enthÄlt einen potenten BET-Binder/-Inhibitor, ein VHL-bindendes Fragment und eine Zehn-Methylen-Spacer-Einheit. GNE-987 kann in PROTAC-AntikÖrperkonjugat (PAC) verwendet werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2417371-71-0
Sample solution is provided at 25 µL, 10mM.
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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].
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
[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.
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