EPZ5676
Catalog #
27625-1
$235
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Description
EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM.
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Synonyms
(2R,3S,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
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Product Data Gallery
Chemical Structure
Product Info
Storage and Usage
Citations
Purity
≥99% by HPLC
Target(s)
Histone Methyltransferase
Formula
C30H42N8O3
MW
562.71 Da
Solubility
≥28.15 mg/ml in DMSO; insoluble in H2O; ≥50.3 mg/ml in EtOH with ultrasonic. For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Long-term storage in solution is not recommended. Not stable in diluted solutions.
CAS Registry #
1380288-87-8
Background
EPZ5676 is a potent inhibitor of DOT1L histone methyltransferase that, according to X-ray crystallographic analysis, occupies the S-adenosyl methionine (SAM) binding pocket of DOT1L and induces conformational changes in DOT1L resulting in the opening of a hydrophobic pocket beyond the amino acid portion of SAM. EPZ5676 has been investigated for the treatment of MLL-rearranged leukemia in multiple studies where results have shown that EPZ5676 inhibits H3K79 methylation and the expression of MLL-fusion target gene and potently kills acute leukemia cell lines bearing MLL translocation.
References
Daigle SR, et al. Blood. 2013 Aug 8;122(6):1017-1025.
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