| Hazard Information | Back Directory | [Uses]
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC)[1]. | [IC 50]
BRD4 (BD1): 4 nM (IC50); BRD4 (BD2): 3.9 nM (IC50); VHL | [References]
[1] Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31. DOI:10.1002/cmdc.201900497 |
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