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. Author manuscript; available in PMC: 2022 Aug 12.
Published in final edited form as: J Med Chem. 2021 Jul 19;64(15):10997–11013. doi: 10.1021/acs.jmedchem.1c00367

Figure 5. Compound 7 exhibits on-target effect of ENL inhibition in MLL-rearranged leukemia cell lines.

Figure 5.

(A) 7 inhibits leukemia cell growth. Cell growth inhibition of 7 at various concentrations in MV4;11, MOLM13, and U2OS cells. Survived cells were calculated as % relative to DMSO treated cells. (B-C) Cellular thermal shift assays in MV4;11 (B) and MOLM13 (C) cells treated with 20 μM 7 at the indicated temperatures. β-actin was used as a loading control. (D) qRT-PCR analysis of HOXA9 and MYC gene expression in MOLM13 cells treated with 7 or the DMSO negative control. (E-F) 7 shows a synergistic effect with JQ1 in MOLM13 cells. (E) 3D synergy distribution of 7 and JQ1. MOLM13 cells were treated with indicated doses of 7 and JQ1 or DMSO for 6 days. Survived cells were calculated as % relative to DMSO treated cells. Synergistic interactions were analyzed using the Combenefit software. (F) GI50 of 7 when co-treated with indicated concentrations of JQ1. Data in (A) and (D) are shown as mean ± SEM, n = 3, two-tailed Student’s t test, ns, not significant, * P < 0.05, ** P < 0.005, *** P < 0.001, **** P < 0.0001. Data in (E) and (F) represent mean ± SEM, n = 3.