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.
Molekulargewicht:
1200.57
CAS Nummer:
[3060730-06-2]
Formel:
C64H95F2N11O7S
Target-Kategorie:
Histone Methyltransferase|||PROTACs
T202458
T202458
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