mouse g9a

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

MS-8709 is a potent and selective G9a/GLP PROTAC Degrader with a DC50(G9a) of 274 nM and a DC50(GLP) of 260 nM. It induces G9a/GLP protein degradation in a concentration-dependent and time-dependent manner via the ubiquitin-proteasome system, without affecting mRNA expression levels. MS-8709 demonstrates superior cell growth inhibition compared to the parent compound UNC0642 in prostate cancer, leukemia, and lung cancer cell models, and exhibits mouse pharmacokinetic characteristics suitable for in vivo efficacy studies.

MS152 is an orally active EHMT2/G9a inhibitor. It can reactivate the maternally silenced PWS genes in brain and liver tissues of a Prader-Willi Syndrome (PWS) mouse model.