A potent inhibitor of DOT1L (IC50 = 0.3 nM); over 100-fold selective over other PMTs; active in cells

SGC0946 – 10 mg

Brand:
Cayman
CAS:
1561178-17-3
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

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.{21195} Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.{21198} 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 (IC50s = 2.6 and 8.8 nM, respectively). SGC0946 is a brominated analog of EPZ004777, an S-adenosylmethionine-competitive inhibitor of DOT1L.{27033} 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.{27033} The negative control, SGC0649, for SGC0956 is also available exclusively through the SGC. You can submit a request to receive the negative control here.  

 

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Description

A potent inhibitor of DOT1L (IC50 = 0.3 nM); over 100-fold selective over other PMTs; active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50s = 2.6 and 8.8 nM, respectively)

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-amine

Synonyms: 

Molecular weight: 618.6

CAS: 1561178-17-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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