| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
Cell lines | Molm13 MLL and A431 cell lines |
Preparation method | The solubility of this compound in DMSO is >31 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-10 μM |
Applications | SGC0946 showed time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation. Quantitative assessment of H3K79me2 levels as measured by automated epifluorescence microscopy in MCF10A cells showed a substantially improved DOT1L inhibitory potency of SGC0946 (IC50 8.8±1.6 nM) compared with EPZ004777 (IC50 84±20nM). A similar observation was made in A431 cells, with IC50s of 2.65 nM and 264nM for SGC0946 and EPZ004777, respectively. |
| 产品描述 | SGC 0946 is a potent small-molecule inhibitor of protein methyltransferase (PMT) DOT1L, a unique protein lysine methyltransferase (PKMT) catalyzing the methylation of histone H3 on Lysine 79 (H3K79), with the half maximal inhibition concentration IC50 value of 0.3 nM [1]. As a brominated analogue of EPZ004777, SGC 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where SGC 0946 reduces the methylation of H3K79 in both MCF10A (IC50: 8.8 nM) and A431 (IC50: 2.65 nM) cells compared with EPZ004777 (IC50: 84 nM and 264 nM respectively). This greatly increased cellular inhibitory potency of SGC 0946 can be attributed to lower off-rate and to improved cell permeability [1]. Reference References: |
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