GSK852 | BET BD2 inhibitor | Probechem Biochemicals

Chemical Structure : GSK852

GSK852 (GSK-852)

Catalog No.: PC-72183Not For Human Use, Lab Use Only.

GSK852 (GSK-852) is a highly potent, second bromodomain (BD2)-selective BET inhibitor with pIC50 7.9 (BRD4 BD2), 1260-fold selectivity over BRD4 BD1.

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Biological Activity

GSK852 (GSK-852) is a highly potent, second bromodomain (BD2)-selective BET inhibitor with pIC50 7.9 (BRD4 BD2), 1260-fold selectivity over BRD4 BD1.
GSK852 demonstrates highly soluble with good in vivo rat and dog pharmacokinetics.

Physicochemical Properties

M.Wt	406.482
Formula	C24H26N2O4
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	(3S)-N5-((1R,3R,5S)-3-hydroxybicyclo[3.1.0]hexan-6-yl)-N7,3-dimethyl-3-phenyl-2,3-dihydrobenzofuran-5,7-dicarboxamide

References

1. Simon C C Lucas, et al. J Med Chem. 2021 Aug 12;64(15):10711-10741.

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GSK852 (GSK-852)

Biological Activity

Physicochemical Properties

References

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