Fig. 3.

Activity of compounds 1–3 on ENL and AF9 in MLL1-r leukemia cells. a–e Levels of ENL, AF9 and β-actin (as a control) in a–d MV4;11 and e Molm-13 cells upon treatment with compounds 1 (a/d/e), 2 (b), and 3 (c) at the specified concentrations for 24 h, showing they induced degradation of ENL with their dose-responsive curves for calculating DC₅₀ shown at right. AF9 levels were not reduced; f time-dependent degradation of ENL in MV4;11 cells by 1 (500 nM); g–i ENL levels in MV4;11 cells upon pre-treatment for 2 h with SGC-iMLLT (Inh, g), thalidomide (Tha, h) and bortezomib (Bor, i) followed by co-treatment with 1 (500 nM) for 24 h, showing these three compounds can dose-dependently inhibit 1-mediated ENL degradation