EPZ005687, CAS 1396772-26-1

Products from BPS Bioscience require a minimum order value above 400€

Background: EPZ005687 is a potent inhibitor of EZH2, an enzymatic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of histone H3 lysine 27 (H3K27), that inhibits EZH2 with Ki of 24 nM, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related EZH1 respectively. EPZ005687 concentration-dependently inhibits the enzymatic activity of PRC2 with IC50 of 54 nM through binding to the S-adenosylmethionine (SAM) pocket of the EZH2 SET domain. Study results have shown that EPZ005687 reduces H3K27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells.

Biological Activity: Potent and selective EZH2 inhibitor with Ki of 24 nM. It exhibits 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

CAS Number: 1396772-26-1

Description: EPZ-005687 is a potent and selective inhibitor of EZH2.

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: EZH2

Biosafety Level: Not applicable (BSL-1)

References: Knutson SK, et al. Nat Chem Biol. 2012 Nov;8(11):890-6.

• Artikelnummer: BPS27624-2
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 27624-2
• Green Labware: Nein
• Verpackungseinheit: 25 mg
• Mengeneinheit: STK