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描述 | There are 18 mammalian HDACs, HDAC 1-11 and sirt 1-7. One of the member, HDAC6 can target specific substrates like HSP90 andα-tubulin which involve in protein trafficking and degradation or cell shape and migration, thus participates in the pathways relating to neurodegenerative diseases, cancer, and immunology. CAY10603 is a highly selective HDAC 6 inhibitor with IC50 value of 0.002nM, also exhibited weaker inhibitory effect on HDAC3 and HDAC 10 with IC50 values of 0.42nM and 90.7nM, respectively. CAY10603 were active against both the Mia Paca-2 and Panc04.03 cell lines at the 100 nM level, and against HupT3 at the 200-300 nM[1]. CAY10603 led growth inhibition of A549 and HCC827 cells at concentration<10μM. CAY10603 induced apoptosis at concentration of 0.16μM and 0.32μM in A549 after 48h treatment. Inhibition of HDAC6 through CAY10603 inactivated the EGFR pathway[2]. HDAC6 inhibition by CAY10603 prevented LPS-induced ɑ-tubulin deacetylation in the lung tissues and exhibited protective effects against LPS-induced acute lung inflammation[3]. | ||
作用机制 | CAY10603 can bind directly to HDAC6 and chelate Zn2+ through its Zn-binding domain.[1][3] |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HMEC | Cytotoxicity assay | 72 h | Cytotoxicity against HMEC after 72 hrs by MTT assay, IC50=1 μM | 18642892 | |
HPDE 6c7 cells | Cytotoxicity assay | 72 h | Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay, IC50=0.5 μM | 18642892 | |
human BxPC3 cells | Proliferation assay | 72 h | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50=1 μM | 18642892 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.20mL 2.24mL 1.12mL |
22.40mL 4.48mL 2.24mL |
参考文献 |
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