CAM833 是一种有效的抑制BRCA2和RAD51之间相互作用的正位抑制剂,对 ChimRAD51 蛋白的Kd为 366 nM。 CAM833 也抑制 RAD51 的寡聚。
产品描述
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization [1].
体外活性
CAM833 (3.125-50 μM; 24 h) causes a concentration-dependent decrease in RAD51 foci and subsequent increase in DNA damage [1]. CAM833 (25 μM) inhibits RAD51 molecular clustering at DNA damage sites [1]. CAM833 (0-50 μM) inhibits DNA repair by homologous recombination [1]. CAM833 (20 μM; 0-72 h) potentiates radiation-induced cell-cycle arrest and increases apoptosis over time [1]. CAM833 (10 μM) causes a dose-dependent growth inhibition that is enhanced when combined with ionizing radiation [1]. CAM833 (20 μM; 96 h) potentiates the growth suppressive effect of PARP1 inhibition in BRCA2 wild-type cells [1]. Cell Cycle Analysis [1] Cell Line: HCT116 cells Concentration: 20 μM Incubation Time: 0-72 h Result: In the control the percentage of cells in the apoptotic subG1 fraction remains below 5% throughout, in the compound-treated cells this rises progressively to peak at 15% at 48 hours.
Cas No.
2758364-02-0
分子式
C26H26ClFN4O5
分子量
528.96
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