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GT-653

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]

Product Specifications

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

Available Sizes

Curated Selection

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