Chemical Structure : I-BET787
CAS No.:
2201082-98-4
I-BET787
(GSK3535787, GSK 3535787)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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321.81
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Formula
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C16H20ClN3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(4-Chloro-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-imidazole-2-yl)-1,3-dimethylpyridin-2(1H)-one
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References
1. David J Hirst, et al. J Med Chem. 2024 Jun 12. doi: 10.1021/acs.jmedchem.4c00959.
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