LCL161 is an IAP family inhibitor which can bind and inhibit both XIAP and cIAP. Treatment with LCL161 could enhance the activity of different proapoptotic signaling pathways[1]. LCL-161 at concentration of 2μM could induce cIAP degradation and activated downstream NFκB in Eμ-Myc cells[2]. Treatment with LCL161 at concentration<10μM for 24h did not significantly affect protein level of XIAP protein level as Smac-mimetic treatment did not degrade XIAP, but can still inhibit the activity of XIAP measured by upregulation of cleaved caspases 9 and 3, in H929, MM1R and MM1S cells. LCL161 at concentration<15μM dose-dependently induced cell death of H929 and MM1S cells primarily driven by activation of the extrinsic apoptotic pathway[3]. Combination of LCL161 (100mg/kg) with nilotinib showed synergistic effects and significantly delayed the onset of disease recurrence in a BCR-ABL-positive leukemia model[1].
作用机制
LCL-161 is a SMAC mimetic which can both disengage IAPs from caspases and induce proteasomal degradation of cIAP-1 and -2.[2]
LCL161 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human AGS cells
2.5 μM
Apoptosis assay
5 days
Induction of sensitization of human AGS cells to conatumumab-induced apoptosis assessed as cell viability at 2.5 uM after 5 days by MTS assay
24093940
human BxPC3 cells
3.3 μM
Cytotoxic assay
5 days
Potentiation of conatumumab-induced cytotoxicity against human BxPC3 cells at 3.3 uM after 5 days by MTS assay
24083782
human Capan1 cells
2.5 μM
Cytotoxic assay
5 days
Potentiation of conatumumab-induced apoptosis in human Capan1 cells at 2.5 uM after 5 days by MTS assay
24093940
human Capan1 cells
2.5 μM
Apoptosis assay
5 days
Potentiation of conatumumab-induced apoptosis in human Capan1 cells at 2.5 uM after 5 days by MTS assay
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