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Cat. Number
E6396
Chemical Name
E6396 EPZ005687 1396772-26-1
CAS Number
1396772-26-1
Mol. Formula
C32H37N5O3
Mol. Weight
539.67
Qty 1
1mg
Qty 2
100mg
Appearance
white powder
Application Notes
≥99%
Solubility
DMSO 2 mg/mL (3.7 mM) Water Insoluble Ethanol Insoluble
Storage condition
-20°C
References

EPZ-005687 is a highly selective inhibitor of mutant EZH2, a histone methyltransferase (HMT) that exhibits point mutations at key residues Tyr641 and Ala677 in non-Hodgkin’s lymphoma and other cancers. EPZ-005687 displays anticancer chemotherapeutic activity through its inhibition of EZH2; this enzyme is responsible for methylation of lysine and arginine residues and controls gene transcription fidelity in cells. Inhibition of mutant EZH2 induces apoptosis.


References

Knutson SK, Wigle TJ, Warholic NM, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6. PMID: 23023262.


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