EPZ5676, CAS 1380288-87-8

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Background: EPZ5676 is a potent inhibitor of DOT1L histone methyltransferase that, according to X-ray crystallographic analysis, occupies the S-adenosyl methionine (SAM) binding pocket of DOT1L and induces conformational changes in DOT1L resulting in the opening of a hydrophobic pocket beyond the amino acid portion of SAM. EPZ5676 has been investigated for the treatment of MLL-rearranged leukemia in multiple studies where results have shown that EPZ5676 inhibits H3K79 methylation and the expression of MLL-fusion target gene and potently kills acute leukemia cell lines bearing MLL translocation.

Biological Activity: EPZ5676 selectively inhibits DOTIL with an IC50 of 0.8 nM, which is 37000-fold greater in selectivity vs. other methyltransferases, including CARM1, EHMT1/2, EZH1/2, PRMT1/2/5/6/8, SETD7, SMYD2/3, and WHSC1/1L1. Inhibits H3K79 methylation in tumors.

CAS Number: 1380288-87-8

Description: EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM.

Purity: ≥98% by HPLC

Solubility: Soluble in DMSO

Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Target: Dot1L

Biosafety Level: Not applicable (BSL-1)

References: Daigle SR, et al. Blood. 2013 Aug 8;122(6):1017-1025.

• Artikelnummer: BPS27625-2
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 27625-2
• Green Labware: Nein
• Verpackungseinheit: 50 mg
• Mengeneinheit: STK