Molecular Formula | C28H40BrN7O4 |
Molar Mass | 618.57 |
Density | 1.48±0.1 g/cm3(Predicted) |
Melting Point | 125-126o C |
Boling Point | 771.5±60.0 °C(Predicted) |
Solubility | DMSO: soluble20mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | 12.39±0.70(Predicted) |
Storage Condition | -20°C |
In vitro study | SGC 0946 is 100-fold more selective than other histone methyltransferases/HMTs. SGC 0946 acts on A431 cells and MCF10A cells, effectively reducing H3K79 dimethylation with IC50 of 2.6 nM and 8.8 nM, respectively, and effectively and selectively kills cells containing MLL translocation. SGC 0946 is more potent than its analog EPZ004777 and serves as an excellent chemical probe for the Study of DOT1L, and further studies of the use of DOT1L inhibitors for cancer treatment. SGC 0946 is 100-fold more selective than other histone methyltransferases/HMTs. SGC 0946 acts on A431 cells and MCF10A cells, effectively reducing H3K79 dimethylation with IC50 of 2.6 nM and 8.8 nM, respectively, and effectively and selectively kills cells containing MLL translocation. SGC 0946 is more potent than its analog EPZ004777 and serves as an excellent chemical probe for the Study of DOT1L, and further studies of the use of DOT1L inhibitors for cancer treatment. |
Hazard Symbols | T - Toxic |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.617 ml | 8.083 ml | 16.166 ml |
5 mM | 0.323 ml | 1.617 ml | 3.233 ml |
10 mM | 0.162 ml | 0.808 ml | 1.617 ml |
5 mM | 0.032 ml | 0.162 ml | 0.323 ml |
biological activity | SGC 0946 is a potent, selective DOT1L methyltransferase inhibitor with an IC50 of 0.3 nM, inhibition of 12 PMTs and DNMT1 activity. SGC 0946 is a potent, selective DOT1L methyltransferase inhibitor with an IC50 of 0.3 nM in a cell-free assay and no activity on a series of 12 PMTs and DNMT1. |
in vitro study | SGC 0946 is 100-fold more selective than other histone methyltransferases/HMTs. SGC 0946 acts on A431 cells and MCF10A cells, effectively reducing H3K79 dimethylation with IC50 of 2.6 nM and 8.8 nM, respectively, and effectively and selectively kills cells containing MLL translocation. SGC 0946 is more potent than its analog EPZ004777 and serves as an excellent chemical probe for the Study of DOT1L, and further studies of the use of DOT1L inhibitors for cancer treatment. SGC 0946 is 100-fold more selective than other histone methyltransferases/HMTs. SGC 0946 acts on A431 cells and MCF10A cells, effectively reducing H3K79 dimethylation with IC50 of 2.6 nM and 8.8 nM, respectively, and effectively and selectively kills cells containing MLL translocation. SGC 0946 is more potent than its analog EPZ004777 and serves as an excellent chemical probe for the Study of DOT1L, and further studies of the use of DOT1L inhibitors for cancer treatment. |
features | Cell-active DOT1L-selective chemical probe. |
Target | TargetValue DOT1L (Cell-free assay) 0.3 nM |
Target | Value |
DOT1L (Cell-free assay) | 0.3 nM |