GNE-987

GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. 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).


Cat. No.: EX-A10356	Purity: >98%

	Chemical structure of GNE-987

For research only, Do not use for Human!

Size	Unit Price (US$)	Stock
50mg	715	In-stock
100mg	1072	In-stock
250mg	1982	In-stock
500mg	3216	In-stock
1g	4900	In-stock
5g	get quote	In-stock

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CAS No.	2417371-71-0
Purity	>98%
Formula	C56H67F2N9O8S2
Mol Weight	1096.313
Color	white to off-white
State	solid
Solubility	soluble in DMSO
Shelf Life	>2 years if stored properly
Storage	Powder 4℃ 1 year; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.
CoA	CoA of GNE-987

Smiles:	O=C([C@H](C[C@@H](O)C1)N1C([C@@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7


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