Compound class:
Synthetic organic
Comment: SGC0946 is a brominated analogue of EPZ004777 and is a DOT1L inhibitor [1]. This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Mechanism Of Action and Pharmacodynamic Effects |
SGC0946 inhibits histone methylation (at H379K) by DOT1L by binding within the S-adenosylmethionine (SAM) cofactor-binding site common to all histone lysine methyltransferases (KMTs). Treatment inhibits methylation of lysine 79 of histone H3 (H3K79), with DOT1L being the only methyltransferase to perform this specific methylation [1]. H3K78me2 (dimethylation) marks are depleted in cell lines expressing MLL rearrangements exposed to SGC0946, and exposure also compromises cell viability [1]. |