产品
编 号:F225218
分子式:C26H30ClN3O4S
分子量:516.05
产品类型
结构图
CAS No: 1808951-93-0
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产品详情
生物活性:
LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.
体外研究:
LP99 disrupts BRD9 interactions with chromatin at a concentration of 0.8 μM. BRD7- and BRD9-NanoLuc luciferase fusion proteins and fluorescently labelled histone H3.3- and H4-HaloTag fusions were expressed in HEK293 cells. The addition of LP99 decreased BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose-dependent manner, with cellular IC50 values in the low micromolar range for both histone. Cytotoxicity tests in U2OS cells for 24 and 72 hours shows the inhibitor to be non-toxic at concentrations of LP99 相关抗体: