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CAS: 329059-55-4
分子式: C28H36N2O4S
分子量: 496.66
英文名称: 
brd7116
2,2,3,3-tetramethyl-n-[4-[4-[(2,2,3,3-tetramethylcyclopropanecarbonyl)amino]phenyl]sulfonylphenyl]cyclopropane-1-carboxamide
n,n'-(sulfonyldi-4,1-phenylene)bis[2,2,3,3-tetramethyl-cyclopropanecarboxamide
用途: BRD7116竞争性地结合到细菌DNA促旋酶, 作用于LSCe 细胞,EC50值为200 nM, 具有非自治性的抗白血病活性。
推荐供应商
货号品牌产品名称规格包装、参考价格
B879562MACKLINBRD7116 ≥99%695元/5mg;   1253元/10mg;   咨询
储存:2-8℃
2286584J&KBRD711699%, 竞争性地结合到细菌DNA促旋酶, 作用于LSCe 细胞665元/5MG;   1140元/10MG;   咨询

基本信息

分子式C28H36N2O4S
分子量496.66
存储条件Freezer -20℃

产品描述

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

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