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GT-653

Chemical Structure : GT-653

CAS No.:

GT-653 (GT653)

Catalog No.: PC-22356Not For Human Use, Lab Use Only.

GT-653 is a potent, selective and effective KDM5B PROTAC degrader based on CPI-455, induces KDM5B degradation via PROTAC mechanism and ubiquitin proteasome system dependent manner.

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Biological Activity

GT-653 is a potent, selective and effective KDM5B PROTAC degrader based on CPI-455, induces KDM5B degradation via PROTAC mechanism and ubiquitin proteasome system dependent manner.
GT-653 (0-20 uM) induced KDM5B degradation and H3K4me3 upregulation in 22RV1 cells, significantly degraded the KDM5B with a degradation rate of 68.35 %, does not affect KDM5A or KDM5C with CRBN.
GT-653 induced KDM5B degradation in a ubiquitin proteasome system dependent manner.
GT-653 treatment upregulated interferon (IFN) response genes in prostate cancer.

Physicochemical Properties

M.Wt 653.61
Formula C32H27N7O9
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

2-(4-(3-cyano-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-5-yl)phenoxy)-N-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)ethoxy)ethyl)acetamide

References

1. Tian Guan, et al. Eur J Med Chem. 2024 May 10:272:116494.

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