| 产品详情 |
| Edit |   |
|---|
| Product Name | SGC0946 |
|---|
| Description | Purity >98%. DOT1L is a protein methyltransferase (PMT). It is the only enzyme known to methylate histone 3 at lysine 79 (H3K79), where it catalyzes mono-, di-, and trimethylation. Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation. SGC0946 is a potent inhibitor of DOT1L (IC50 = 0.3 nM) developed by the Structural Genomics Consortium (SGC) . It is over 100-fold selective over other PMTs. It is active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50 s = 2.6 and 8.8 nM, respectively). SGC0946 is a brominated analog of EPZ004777, an S-adenosylmethionine-competitive inhibitor of DOT1L. Both SGC0946 and EPZ004777 selectively kill mixed lineage leukemia (MLL) cells, in which DOT1L is aberrantly localized via interaction with an oncogenic MLL fusion protein. |
|---|
| Size | n/a |
|---|
| Concentration | n/a |
|---|
| Applications | n/a |
|---|
| Other Names | 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-Beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
|---|
| Gene, Accession, CAS # | CAS: 1561178-17-3 |
|---|
| Catalog # | LS-H9910 |
|---|
| Price | |
|---|
| Order / More Info | SGC0946 from LIFESPAN BIOSCIENCES INC. |
|---|
| Product Specific References | n/a |
|---|
| 产品资料 |
|
|