BRD7116

基本信息

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BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity. IC50 value: 200 nM (EC50, for LSCe cells) Target: DNA gyrase BRD7116 is a bis-aryl sulfone, shows evidence of stroma-mediated anti-LSCe activity. BRD7116 exhibits an EC50 of 200 nM for LSCe cells in co-culture, whereas it displays limited activity against normal HSPCs and AML cell lines (～50% inhibition at 20 μM). BRD7116 also shows activity against patient-derived, primary human leukemia cells. [1] BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs.

靶点（IC50 & Targe）

DNA gyrase

参考文献

[1]. Hartwell KA, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells. Nat Chem Biol. 2013 Dec;9(12):840-848