GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC 50 =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 (IC 50 =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).
性状
Solid
IC50 & Target[1][2]
BRD4 (BD1) 4.7 nM (IC50) BRD4 (BD2) 4.4 nM
体外研究(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. GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.
溶解度数据
In Vitro: DMSO : 150 mg/mL (136.82 mM; Need ultrasonic)配制储备液