85-2072-74 Ezh2 Inhibitor II, EI1(Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI, 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide) 10mg CAS No:1418308-27-6 217349
A cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2/SUZ12/EED/AEBP2/RbAP48) HMTase activity (IC50/substrate = 15nM/H3K27me021-44 and 13nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1uM) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50 = 1.34uM) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50 >100uM). Shown to suppress cellular H3K27 dimethylation and trimethylation (1 to 10uM) in DLBCL cultures and exhibit antiproliferation activity against DLBCL cell lines with wt or mutant Ezh2 (3.3uM to 10uM).
Molecular Formula:C₂₃H₂₆N₄O₂
Primary Target:Ezh2/PRC2
Molar Mass:390.5
Solubility:DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
