A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM); inhibits the H3K79 methylation in various human leukemia cell lines (IC50s = 3-5 nM)

EPZ5676 – 5 mg

Brand:
Cayman
CAS:
1380288-87-8
Storage:
-20
UN-No:
Non-Hazardous - /

DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias.{21198,21195} EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases.{26366,26367} In various human leukemia cell lines, EPZ5676 has been shown to inhibit the methylation of lysine 79 on histone 3 (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression (IC50s = 53-67 nM).{26366} It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM – 1.3 µM).{26366} Continuous intravenous infusion of EPZ5676 at a dose of 35 mg/kg has been reported to cause complete and sustained tumor regression in a rat xenograft model of MLL-rearranged leukemia.{26366}  

 

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Description

A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM); inhibits the H3K79 methylation in various human leukemia cell lines (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression and inhibiting proliferation; intravenous infusion of EPZ-5676 at a dose of 35 mg/kg can regress tumors in a rat xenograft model of MLL-rearranged leukemia

Formal name: 9-[5-deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine

Synonyms: 

Molecular weight: 562.7

CAS: 1380288-87-8

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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