A potent DOT1L inhibitor (IC50 = 400 pM) that selectively kills (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model; accelerates the reprogramming of somatic cells into induced pluripotent stem cells

EPZ004777 (formic acid salt) – 500 µg

Brand:
Cayman
CAS:
1338466-77-5
Storage:
-20
UN-No:
Non-Hazardous - /

DOT1L is a protein methyltransferase. It is the only enzyme known to methylate histone 3 at lysine 79, 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} EPZ004777 is a potent inhibitor of DOT1L (IC50 = 400 pM) that selectively kills mixed lineage leukemia (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model.{30897,30896,30898,27033} It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.{30897} DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.{30334}  

 

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Description

A potent DOT1L inhibitor (IC50 = 400 pM) that selectively kills (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model; accelerates the reprogramming of somatic cells into induced pluripotent stem cells

Formal name: 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, monoformic acid salt

Synonyms: 

Molecular weight: 585.7

CAS: 1338466-77-5

Purity: ≥98%

Formulation: A crystalline solid

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

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