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Description: BRD7116 is a novel, potent and selective Inhibitor of leukemia stem cell (LSC) activity with EC50 of 200 nM. It exhibits > 100-fold selectivity for LSCs over normal hematopoietic stem cells. Efforts to develop more effective therapies for acute leukemia may benefit from high-throughput screening systems that reflect the complex physiology of the disease, including leukemia stem cells (LSCs) and supportive interactions with the bone marrow microenvironment. The therapeutic targeting of LSCs is challenging because LSCs are highly similar to normal hematopoietic stem and progenitor cells (HSPCs) and are protected by stromal cells in vivo.
References: Nat Chem Biol. 2013 Dec; 9(12):840-848.
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