| 供货周期： | 一周 |
| 品牌： | 爱必信 |
| 规格： | >98% |
| 货号： | abs811037 |
| CAS号： | 1262849-73-9 |
| 公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!
抑制剂描述： 产品名称：CCT241533 产品别名：见爱必信官网 英文别名：CCT241533 靶点：Chk CAS：1262849-73-9 纯度：>98% 外观：见爱必信官网 保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述： CCT241533 is a potent and selective Inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. 溶解性：10 mM in DMSO 体外研究： CCT241533 hydrochloride inhibits CHK2 with an IC50 of 3 nM and shows minimal cross reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms that CCT241533 binds to CHK2 in the ATP pocket. CCT241533 blocks CHK2 activity in human tumor cell lines in response to DNA damage, as demonstrated by inhibition of CHK2 autophosphorylation at S516, band-shift mobility changes and HDMX degradation. CCT241533 does not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, CCT241533 significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal is seen with a PARP inhibitor alone and this activation is abolished by CCT241533. The cytotoxicity of CCT241533 in HT-29, HeLa and MCF-7, measured as the growth inhibitory IC50(GI50) by SRB assay, is 1.7, 2.2 and 5.1 μM, respectively. CCT241533 hydrochloride is a potent CHK2 inhibitor (IC50=3 nM), with selectivity (63-fold) over CHK1(IC50=190 nM) and low hERG inhibition (IC50=22 μM). 体内研究：
产品信息订购：
|
相关产品
工商信息
信息已认证
联系方式
详细地址
关注
拨打电话
留言咨询
