GNE-987是一种高活性的嵌合体BET降解剂。GNE-987显示皮摩尔细胞BRD4降解活性(在EOL-1AML细胞系中，DC50=0.03nM)。GNE-987与BRD4的BD1和BD2结合，具有低纳米摩尔亲和力(IC50分别为4.7和4.4nM)。它包含一个有效的BET结合剂/抑制剂、一个VHL结合片段和一个十个亚甲基间隔基部分。GNE-987用于PROTAC-Antibody偶联物(PAC)中。
货号:ajcx30734
CAS:2417371-71-0
分子式:C56H67F2N9O8S2
分子量：1096.31
溶解度:DMSO: 150 mg/mL (136.82 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.