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GNE-064

Chemical Structure : GNE-064

CAS No.: 1997321-20-6

GNE-064 (GNE064)

Catalog No.: 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.

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5 mg $258 In stock
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100 mg $1380 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 327.388
Formula C17H21N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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