GNE-987 |
| رقم الكتالوجGC60883 |
GNE-987 عبارة عن PROTAC متصل بواسطة روابط لـ von Hippel-Lindau و BRD4يعرض GNE-987 نشاط تحلل خلية البيكومولار BRD4 (DC50 = 0.03 نانومتر لخط خلايا EOL-1 AML)يرتبط GNE-987 بشكل متساوٍ بنطاقات BD1 و BD2 من BRD4 مع تقاربات نانوية منخفضة (IC50 = 4.7 و 4.4 نانومتر ، على التوالي)يشتمل GNE-987 على مادة رابطة / مثبط BET قوية ، وجزء ربط VHL ، وجزء مباعد من عشرة ميثيلينيمكن استخدام GNE-987 في PROTAC-Antibody Conjugate (PAC)
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *