KPT-276
| CAS号 | 1421919-75-6 | 货号 | BCP09428 |
| 中文名 | KPT-276 | ||
| 英文名 | KPT-276 | ||
| 中文别名 | |||
| 英文别名 | KPT 276;KPT276; | ||
| 分子式 | C16H10F8N4O | 分子量 | 426.26 |
| 生物活性 | KPT-276, analog of KPT-185, is an orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of CRM1. IC50 value: Target: CRM1 in vitro: A selective inhibitor of nuclear export compound KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1. The viability of 12 HMCLs treated with KTP-276 was significantly reduced. KPT-276 also actively induced apoptosis in primary MM patient samples. In gene expression analyses, two genes of probable relevance were dysregulated by KPT-276: cell division cycle 25 homolog A (CDC25A) and bromodomain-containing protein 4 (BRD4), both of which are associated with c-MYC pathway . Inhibition of CRM1 by two novel selective inhibitors of nuclear export (SINE), KPT-185 and KPT-276, in MCL cells resulted in significant growth inhibition and apoptosis induction. KPT-185 also induced CRM1 accumulation in the nucleus, resulting in CRM1 degradation by the proteasome . | ||
| 信号通路 | Ion Channel/Membrane Transporter | ||
| 靶 点 | CRM1 | ||
结构式
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