BRD7116 is a selective inhibitor of leukemia stem cells.
BRD7116 is a selective inhibitor of leukemia stem cells. BRD7116 had an EC50 of 200 nM for the leukemia stem cell (LSC)-enriched fraction of cells isolated from the bone marrow of leukemic animals in co-culture compared to ~50% inhibition at 20 μM against normal hematopoietic stem and progenitor cells (HSPCs) and AML cell lines. BRD7116 selectively targeted LSCe cells by cell-autonomous and cell-non-autonomous mechanisms. The exact mechanism is not known, but involved in impairing of the stroma′s ability to support leukemia cells, and inducing transcriptional changes consistent with myeloid differentiation.
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