2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. EPZ004777 formate

EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.

For research use only. We do not sell to patients.

EPZ004777 formate

EPZ004777 formate Chemical Structure

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EPZ004777 formate Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia[1][2][3].

IC50 & Target[1]

DOT1L

0.4 nM ()

Molecular Weight

585.70

Formula

C29H43N7O6
SMILES

O=CO.NC1=NC=NC2=C1C=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN(C(C)C)CCCNC(NC(C=C4)=CC=C4C(C)(C)C)=O)O3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EPZ004777 formate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EPZ004777 formateHistone MethyltransferaseApoptosisDOT1LEPZ004777MLLLeukemiaH3K79 methylationHistone methyltransferase inhibitorTargeted therapyGene expressionIn vivo modelInhibitorinhibitorinhibit

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