SGC0946

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SGC0946

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Cat No: 13967

Biochemicals - Small Molecule Inhibitors

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 gen...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-?-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Correlated keywords:

methyltransferase epigenetic histone modification chromatin research inhibit inhibitor DOT1L protein PMTs enzyme methylate 3 three lysine 79 H3K79 catalyze monomethylation dimethylation trimethylation transcriptional gene DNA deoxyribonucleic acid damage repair cell cycle regulation A431 MCF10A bromine brominated analogs S-adenosylmethionine-competitive SAM-competitive EPZ004777 kills mixed lineages leukemia MLL cancers oncogenic fusion SGC 0946 Structural Genomic Consortium

Product Overview:
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.

Size	5 mg
Shipping	dry ice
CAS Number	1561178-17-3
Molecular Formula	C₂₈H₄₀BrN₇O₄
SMILES	CC(C)(C)C1=CC=C(NC(NCCCN(C(C)C)C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C(Br)=C3)O2)=O)C=C1
Molecular Weight	618,6
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

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