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Chemical Structure : GNE-235
Catalog No.: PC-21166Not For Human Use, Lab Use Only.
GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.
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GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.
GNE-235 displays >20-fold selectivity over PBRM1(5), SMARCA2 and SMARCA4 in BROMOscan assays.
GNE-235 has binding KD value of 1.1 uM against PBRM1(2) in ITC assays, >30-fold selectivity over PBRM1(4) and PBRM1(3).
GNE-235 also shows clear profiles in the nuclear receptor assays, and the low-level PXR activation.
| M.Wt | 244.30 | |
| Formula | C13H16N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Andrea G Cochran, et al. J Med Chem. 2023 Sep 13. doi: 10.1021/acs.jmedchem.3c01149.
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