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GSK983

Chemical Structure : GSK983

CAS No.: 2984100-87-8

GSK983 (GSK-983;GSK 983)

Catalog No.: PC-35668Not For Human Use, Lab Use Only.

GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK983 (GSK-983) is a potent, cell penetrant PCAF/GCN5 PROTAC, induces concentration-dependent degradation of PCAF and GCN5 in THP1 cells with DC50 value of 1.5 nM and 3 nM, respectively
GSK983 also potently induces robust and concentration-dependent degradation of PCAF and GCN5 in both macrophages and monocyte-derived dendritic cells (DCs).
GSK983 potently modulate the expression of multiple inflammatory mediators in LPS-stimulated macrophages and dendritic cells.

Physicochemical Properties

M.Wt 895.856
Formula C45H51BrN8O7
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

4-(5-((5-bromo-1-methyl-6-oxo-1,6-dihydropyridazin-4-yl)amino)-1-methylpiperidin-3-yl)-N-(3-((4-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)propyl)phenyl)(methyl)amino)propyl)-N-methylbenzamide

References

1. Bassi ZI, et al. ACS Chem Biol. 2018 Oct 19;13(10):2862-2867.

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