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BRD7116 is a bis-aryl sulfone that acts as a selective inhibitor of leukemia stem cell activity. It exhibits an EC50 value of 200 nM for leukemia stem cells isolated from the bone marrow of leukemic animals in co-culture but does not affect normal hematopoietic stem cells or AML cell lines (EC50s = 20 µM).1 Its exact mechanism is not well understood but is thought to involve impairment of the stroma’s ability to support leukemia stem cells by inducing transcriptional changes consistent with myeloid differentiation.1
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