HDAC3 degrader GS-1

Chemical Structure : HDAC3 degrader GS-1

Catalog No.: PC-26370Not For Human Use, Lab Use Only.

GS-1 is a potent, selective HDAC3 degrader with DC50 of 1.24 uM in THP-1 cells, shows minimal degradation of HDAC1 or HDAC2 at 5 uM.

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Biological Activity

GS-1 is a potent, selective HDAC3 degrader with DC50 of 1.24 uM in THP-1 cells, shows minimal degradation of HDAC1 or HDAC2 at 5 uM.
GS-1 shows covalent binding with HDAC3 at Lys367.
GS-1 disrupts inflammasome activation through selective HDAC3 degradation in macrophages.
GS-1 (15 mg/kg, intraperitoneally) potent protection against systemic inflammation in LPS-induced endotoxic shock model.
GS-1 (15 mg/kg, i.p.) significantly attenuated weight loss and colonic inflammation in DSS-induced colitis model.

Physicochemical Properties

M.Wt	883.19
Formula	C54H70N6O5
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	N1-(2-aminophenyl)-N7-(4-(4-((2S,4aS,6aS,6bR,8aR,12aS,12bR,14bR)-11-cyano-2,4a,6a,6b,9,9,12a-heptamethyl-10,13-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,12b,13,14b-octadecahydropicene-2-carbonyl)piperazin-1-yl)phenyl)heptanediamide

References

1. Huanhuan Qin, et al. J Med Chem. 2026 Mar 11. doi: 10.1021/acs.jmedchem.5c02513.