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Apexbio Technology LLC SGI-1027 1020149-73-8 10mM (in 1mL DMSO)
Supplier: Apexbio Technology LLC B16225.1
SGI-1027 (CAS 1020149-73-8) is a small-molecule inhibitor of DNA methyltransferases (DNMTs) exhibiting IC50 values of 12 5 M for DNMT1 8 M for DNMT3A and 7 5 M for DNMT3B It acts by competitively inhibiting the cofactor Ado-Met binding site rather than the DNA substrate site resulting in reduced DNMT activity and subsequent inhibition of DNA methylation SGI-1027 suppresses both mammalian and bacterial DNMTs affecting endogenous and recombinant forms In cancer cell models it induces demethylation of CpG islands in gene promoter regions leading to reactivation of silenced tumor suppressor genes such as P16 and TIMP3 and promotes DNMT1 degradation via the proteasome pathway SGI-1027 is utilized in epigenetics research to study DNA methylation dynamics and gene reactivation
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