BRD7116
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 10mg | ¥380.00 | 10-15工作日发货 | |
| 25mg | ¥760.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
BRD7116, a bis-aryl sufone, acts as a selective inhibitor of leukemia stem cell activity by directly acting on the stromal cells to inhibit cobblestone formation [1,2].
BRD7116 displayed cell-non-autonomous anti-leukemia activity. In leukemia stem cells isolated from the bone marrow of leukemic animals in co-culture, BRD7116 exhibited an EC50 of 200 nM. BRD7116 displayed limited activity against normal HSPCs and AML cell lines with EC50s about 20 μM. BRD7116 showed activity against patient-derived primary human leukemia cells. Treatment of LSCe cells with BRD7116 induced transcriptional changes. The mechanism by which BRD7116 impaired the stroma’s ability to support leukemia cells has remained an important issue for future determination [1].
References:
[1] Hartwell K A, Miller P G, Mukherjee S, et al. Niche-based screening identifies small-molecule inhibitors of leukemia stem cells[J]. Nature chemical biology, 2013, 9(12): 840-848.
[2] Sachlos E, Kerstetter-Fogle A. Research Highlights: Highlights from the latest articles in regenerative medicine[J]. Regenerative medicine, 2014, 9(2): 145-147.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 329059-55-4 |
| 分子式 | C28H36N2O4S |
| 分子量 | 496.7 |
| 化学名称 | N,N'-(sulfonyldi-4,1-phenylene)bis[2,2,3,3-tetramethyl-cyclopropanecarboxamide |
| 溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| SMILES | O=S(C1=CC=C(NC(C2C(C)(C)C2(C)C)=O)C=C1)(C3=CC=C(NC(C4C(C)(C)C4(C)C)=O)C=C3)=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | BRD7116 与细菌 DNA 回旋酶竞争性结合,对 LSCe 细胞的 EC50 值为 200 nM,具有细胞非自主抗白血病活性。 IC50 值:200 nM(EC50,用于 LSCe 细胞) 靶点DNA 回旋酶 BRD7116 是一种双芳基砜,显示出基质介导的抗 LSCe 活性。在共培养中,BRD7116 对 LSCe 细胞的 EC50 值为 200 nM,而对正常 HSPCs 和 AML 细胞系的活性有限(20 μM 时抑制率约为 50%)。BRD7116 对源自患者的原发性人类白血病细胞也有活性。 BRD7116 通过对基质细胞的非细胞自主效应以及细胞自主诱导 LSCs 中的髓系分化基因来抑制 LSCs。 |



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