LP99 是一种表观遗传探针,可破坏 BRD7 和 BRD9 与细胞中染色质的结合。它是一种选择性的 BRD7 和 BRD9 溴结构域抑制剂,对 BRD9 的Kd为 99 nM。
产品描述
LP99 is an epigenetic probe. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells. LP99 is an effective and selective inhibitor of the BRD7 and BRD9 bromodomains (Kd: 99 nM against BRD9).
体外活性
LP99 (0.8 μM) disrupts BRD9 interactions with chromatin. 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. LP99 inhibits IL-6 secretion from THP-1 cells in a dose-dependent manner. Cytotoxicity tests in U2OS cells for 24 and 72 hours display the inhibitor to be non-toxic at concentrations of<33 μM .
Cas No.
1808951-93-0
分子式
C26H30ClN3O4S
分子量
516.05
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years