MilliporeSigma™ Calbiochem™ Ezh2 Inhibitor II, EI1

Description

A cell-permeable indolocarboxamide compound

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 = 15 nM/H3K27me0_21-44 and 13 nM/H3K27me2_21-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1μM) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC₅₀ = 1.34μM) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC₅₀ >100μM). Shown to suppress cellular H3K27 dimethylation and trimethylation (1 to 10μM) in DLBCL cultures and exhibit antiproliferation activity against DLBCL cell lines with wt or mutant Ezh2 (3.3μM to 10μM).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Specifications

• Color: White
• Description: 98% by HPLC
• Target Proteins: Ezh2/PRC2
• Molecular Formula: C₂₃H₂₆N₄O₂
• Formula Weight: 390.5g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 10 mg