PROTAC G9a/GLP degrader 1

PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP) . PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775) ; Blue: VHL ligand (HY-125845) ; Black: Linker (HY-140468) ) [1].

Product Specifications

UNSPSC

12352005

Target

GLP Receptor; Histone Methyltransferase; PROTACs

Related Pathways

Epigenetics; GPCR/G Protein; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(CCOCCOCCOCCNC(C1=CC=C(C=C1)NC([C@H](CCC2CC2)NC(C3=C(C4=C(N3)CC(C)(C)CC4=O)C)=O)=O)=O)N[C@H](C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)=O)C(C)(C)C

Molecular Formula

C57H76N8O11S

Molecular Weight

1081.33

References & Citations

[1]Mukherjee A, et al. A Novel PROTAC G9a/GLP Degrader that Inhibits, Similar to G9a siRNA, the Migration of MCF-7 Breast-Cancer Cells without Affecting Proliferation. J Med Chem. 2025 Sep 11;68 (17) :18258-18271.