MS8709 

MS8709 (10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 (10) is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker)^[1].

MS8709 (10) induces significant degradation of G9a and GLP at both 0.3 and 3 µM. Most notably, compound 10 (with an 11-carbon linker) induced more than 70% of G9a and around 50% of GLP degradation at 0.3 µM and complete degradation for both proteins at 3 µM^[1].
MS8709 (10, 1 μM, 24 h) induces G9a/GLP degradation in a VHL- and UPS-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1200.57

C₆₄H₉₅F₂N₁₁O₇S

O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCCNC(CCCN2CCC(NC3=C4C=C(OC)C(OCCCN5CCCC5)=CC4=NC(N6CCC(F)(F)CC6)=N3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Julia Velez, et al. Discovery of the First-in-class G9a/GLP PROTAC Degrader. BioRxiv. Posted February 29, 2024.