SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 (2010) Cancer Res
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SGC0946 - DOT1L inhibitor. CAS# 1561178-17-3 60287 (2010) Cancer ResSGC0946, CAS No. 1561178 17 3, is a highly potent and selective inhibitor of DOT1L methyltransferase. It selectively blocks binding of the cofactor, S adenosylmethionine, to DOT1L, and inhibits the enzyme with an IC50 of 0. 3 nM in a radioactive enzyme assay and is over 100 fold selective for other histone methyltransferases HMTs. SGC0946 potently reduces H3K79 dimethylation with cellular IC50 of 2. 6 nM in A431 cells, and 8. 8 nM in MCF10A cells,
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