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Chemical Structure : GNE-064
CAS No.: 1997321-20-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $358 | In stock | |
| 25 mg | $558 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 327.388 | |
| Formula | C17H21N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-1-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)-2-methylpiperazin-1-yl)ethan-1-one |
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1. Taylor AM, et al. J Med Chem. 2022 Aug 5. doi: 10.1021/acs.jmedchem.2c00662.
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