Name: GNE-987
Brand: TargetMol
SKU: T11441
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

1 mg

¥ 4,950

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5 mg

¥ 11,200

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10 mg

¥ 17,800

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生物活性

产品描述	GNE-987 is a highly active chimeric BET degrader. 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 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line).
靶点活性	VHL:, BRD4 BD2:4.4 nM, BRD4 BD1:4.7 nM
体外活性	GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins.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.

化学信息

分子量	1096.31
分子式	C₅₆H₆₇F₂N₉O₈S₂
CAS No.	2417371-71-0
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
密度	1.40 g/cm3 (Predicted)