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Chemical Structure : I-BET787
Catalog No.: PC-22527Not For Human Use, Lab Use Only.
I-BET787 (GSK3535787) is potent, efficient pan-BET bromodomain inhibitor with pIC50 of 7.1/5.9 for BRD4 BD1/BD2, respectively.
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I-BET787 (GSK3535787) is potent, efficient pan-BET bromodomain inhibitor with pIC50 of 7.1/5.9 for BRD4 BD1/BD2, respectively.
I-BET787 (GSK3535787) demonstrates >500-fold selectivity over 26 bromodomains tested, apart from BAZ2A (20–40-fold) and CREBBP/EP300 (80–160-fold).
I-BET787 (GSK3535787) inhibits human whole blood MCP-1 with an pIC50 value of 6.9, inhibits LPS-stimulated hWB IL-6 with pIC50 of 6.5.
I-BET787 (GSK3535787) demonstrates efficacy in a mouse model of inflammation and suitable properties for both oral and intravenous (IV) administration.
| M.Wt | 321.81 | |
| Formula | C16H20ClN3O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. David J Hirst, et al. J Med Chem. 2024 Jun 12. doi: 10.1021/acs.jmedchem.4c00959.
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