GT-653

• Description :

  GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B) . GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433) ; Black: Linker (HY-W004896) ; Blue: E3 ligase ligand (HY-103596) ) [1]

• UNSPSC :

  12352005

• Target :

  Histone Demethylase; PROTACs

• Type :

  Reference compound

• Related Pathways :

  Epigenetics; PROTAC

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/gt-653.html

• Purity :

  99.84

• Solubility :

  10 mM in DMSO

• Smiles :

  N#CC1=C2NC(C3=CC=C(C=C3)OCC(NCCOCCOC4=CC=CC5=C4C(N(C5=O)C6CCC(NC6=O)=O)=O)=O)=CC(N2N=C1)=O

• Molecular Formula :

  C32H27N7O9

• Molecular Weight :

  653.60

• References & Citations :

  [1]Guan T, et al., Discovery of an efficacious KDM5B PROTAC degrader GT-653 up-regulating IFN response genes in prostate cancer. Eur J Med Chem. 2024 May 10;272:116494.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported