Merck SGC3027
PRMT7 선택적 세포 활성 억제제로서 SGC3027은 세포 내에서 환원효소에 의해 활성 성분 SGC8158로 전환되는 프로드럭입니다. H2B 메틸화에 대해 IC50 < 2.5 nM의 강력한 억제 활성을 가지며, 다른 히스톤 메틸트랜스퍼라아제 대비 40배 이상 선택성을 보여줍니다. C2C12 세포에서 HSP70 메틸화를 IC50 1.3 μM으로 억제합니다.
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Merck SGC3027
SGC3027 is a selective and cell-active inhibitor of protein arginine N-methyltransferase (PRMT7).
It is a pro-drug of the active component SGC8158, which is produced in the cell by reductases.
SGC8158 inhibits PRMT7 with an IC50 < 2.5 nM for methylation of H2B (23–37) and shows >40-fold selectivity over other histone methyltransferases and non-epigenetic targets.
SGC3027 inhibited the methylation of HSP70 in cellular assays using C2C12 cells with an IC50 of 1.3 μM.
The closely related SGC3027N is significantly less active and serves as a control compound for cellular studies.
화학명
N-(4-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)butyl)-N-((4′-chloro-[1,1′-biphenyl]-3-yl)methyl)-3-methyl-3-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dien-1-yl)butanamide
또는 5′-S-[4-[(N-(3-(2,4,5-trimethyl-3,6-dioxo-cyclohexa-1,4-dienyl)-3-methyl)butyryl)-(N-(4′-chloro-biphenyl-3-ylmethyl)amino]butyl]-5′-thioadenosine
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