| Bioactivity | 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] |
| Formula | C32H27N7O9 |
| Molar Mass | 653.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |