GNE-064 | BRG1/BRM inhibitor | Probechem Biochemicals

Chemical Structure : GNE-064

CAS No.: 1997321-20-6

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GNE-064 (GNE064)

货号: PC-49210Not For Human Use, Lab Use Only.

GNE-064 (GNE064) is a potent, selective, and orally bioavailable inhibitor of the bromodomains of SMARCA2 (BRM), SMARCA4 (BRG1) and PBRM1 (polybromo-1) bromodomain 5 (PBRM1(5)) with IC50 of 10 nM, 16 nM and 18 nM, respectively.

规格	价格	库存
5 mg	￥2280	In stock
10 mg	￥3580	In stock
25 mg	￥5580	In stock
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100 mg		Get quote

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生物&药学活性

GNE-064 (GNE064) is a potent, selective, and orally bioavailable inhibitor of the bromodomains of SMARCA2 (BRM), SMARCA4 (BRG1) and PBRM1 (polybromo-1) bromodomain 5 (PBRM1(5)) with IC50 of 10 nM, 16 nM and 18 nM, respectively.
GNE-064 exhibits modest affinity for PBRM1(2) (IC50, 490 nM), and low micromolar affinity for BRD7 and BRD9, >250-fold selective for SMARCA2, SMARCA4, and PBRM1(5) compared to all nonfamily VIII bromodomains.
GNE-064 showed sub-μM activity (IC50=0.1 uM) in an engineered cellular target-engagement assay, had highly soluble, and demonstrated promising stability in hepatocytes.

物理化学性质&存储条件

分子量	327.388
分子式	C17H21N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-1-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)-2-methylpiperazin-1-yl)ethan-1-one

参考文献

1. Taylor AM, et al. J Med Chem. 2022 Aug 5. doi: 10.1021/acs.jmedchem.2c00662.

GNE-064 (GNE064)

生物&药学活性

物理化学性质&存储条件

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GNE-064 (GNE064)

生物&药学活性

物理化学性质&存储条件

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