| SGC0946 |
| 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4- |
| (CAS 1561178-17-3) |
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| Description： |
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 Structural Genomics Consortium laboratories. It is over 100-fold selective over other PMTs. It is active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50s = 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.
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| Product No. |
KT00829 |
| Product Name |
SGC0946 |
| Synonyms |
SGC-0946;SGC 0946 |
| Formal Name |
5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4- |
| CAS Number |
1561178-17-3 |
| Molecular Formula |
C28H40BrN7O4 |
| Formula Weight |
618.6 |
| Formulation |
A crystalline solid |
| Purity |
98%min |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
| Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
| Price & Availability |
In Stock. Price Negotiated. |
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| Related Products： |
Dot1L (human recombinant)
EPZ5676
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