EPZ005687

Research use only, not for human use.

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay.

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

EPZ005687 shows concentration-dependent inhibition of PRC2 enzymatic activity with an IC50?value of 54±5 nM. EPZ005687 specifically inhibits H3K27 methylation in lymphoma cells. EPZ005687 has a notable effect on proliferation of the EZH2Y641F-bearing cell line. EPZ005687 decreases proliferation in mutant but not wild-type EZH2 lymphoma cells. EPZ005687 (0.5, 1, 5 and 10 μM) induces an obvious apoptosis of U937 cells in a dose-dependent manner. EPZ005687 inhibits obviously the proliferation of U937 cells but has weak effect on the proliferation of NBMCD34+ cells. EPZ005687 induces G1 phase blocking and decreases the percentage of cells in S phase in U937 cells. In addition, EPZ005687 produces obviously depletion of H3K27 methylation in U937 cells, but hardly has effect on the H3K27 methylation of NBMCD34+ cells.

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Chromatin/Epigenetic

HMTase

EZH2

Cancer

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1396772-26-1

539.67

C32H37N5O3

>98% (HPLC)

DMSO: 2 mg/mL (3.7 mM)

CC1=CC(C)=C(CNC(=O)C2=C3C=NN(C4CCCC4)C3=CC(=C2)C2=CC=C(CN3CCOCC3)C=C2)C(=O)N1

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(-20℃)

With Ice Pack

≥ 2 years