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GSK785

Chemical Structure : GSK785

CAS No.: 3053860-48-0

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GSK785 (GSK-785)

Catalog No.: PC-26244Not For Human Use, Lab Use Only.

GSK785 (GSK-785) is a BRD2/4-selective bivalent BET I nhibitor with pIC50 of 7.9 and 8.5 in PPI assays against the CRDA parameters, shows pIC50 of 7.4 in the hWB MCP1 assay, 125-fold selectivity for BRD2 over BRD3, 13-fold selectivity for BRD2 over BRD4, and 10-fold selectivity for BRD4 over BRD3.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK785 (GSK-785) is a BRD2/4-selective bivalent BET inhibitor with pIC50 of 7.9 and 8.5 in PPI assays against the CRDA parameters, shows pIC50 of 7.4 in the hWB MCP1 assay, 125-fold selectivity for BRD2 over BRD3, 13-fold selectivity for BRD2 over BRD4, and 10-fold selectivity for BRD4 over BRD3.

Physicochemical Properties

M.Wt 538.69
Formula C33H38N4O3
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

(R)-7-(7-(((R)-1,3-Dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]azepin-7-yl)methyl)-2,7-diazaspiro[3.5]nonane-2-carbonyl)-1,3-dimethyl-1,3-dihydro-2H-benzo[d]azepin-2-one

References

1. Rianjongdee F, et al. J Med Chem. 2026 Jan 22;69(2):895-917.

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