Sirtuin (Sirt) 1 and 2 are members of the NAD+-dependent class III histone deacetylase family that are involved in various cellular events, such as transcriptional silencing, chromatin remodeling, and lifespan duration. Salermide is a potent inhibitor of both Sirt1 and Sirt2. It dose-dependently inhibited human Sirt1 protein with 80% inhibition at 90μM. Salermide shows more efficient inhibitory effect on Sirt2 with 80% inhibition at 25μM. Treatment with 100μM Salermide for 24h induced the decrease of cell numbers in cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231) primary malignancies, but not in non-tumorigenic MRC5 cells. The IC50 values of Salermide in MOLT4, MDA-MB-231 and SW480 cancer cells were around 20, 110, and 100 μM, respectively. After 72-h incubation with 100 μM Salermide, only 10% of KG1A cells and 50% of Raji and K562 cells were viable. An increase of cytosolic-activated caspase 3 and a decrease of mitochondrial-cytochrome c were observed in Salermide-treated cells 2h post treatment. Twenty-four-hour incubation of 25 and 100μM Salermide induced slight tubulin acetylation in MOLT4, MDA-MB-231 and SW480 cells. Intraperitoneal injection of 100μM Salermide over 34 days in nude mice showed no apparent toxicity as monitored by diet consumption, body-weight gain, and postural and behavioral changes[2].
Salermide 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
30P cells
Cytotoxicity assay
72 h
Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay, CC50=41 μM
23189967
30PT cells
Cytotoxicity assay
72 h
Cytotoxicity against human 30PT cells after 72 hrs by celltiter-glo luminescent assay, CC50=36.5 μM
23189967
CRC 1.1 cells
Cytotoxicity assay
72 h
Cytotoxicity against human CRC 1.1 cells after 72 hrs by celltiter-glo luminescent assay, CC50=9.7 μM
23189967
CRO cells
Cytotoxicity assay
72 h
Cytotoxicity against human CRO cells after 72 hrs by celltiter-glo luminescent assay, CC50=6.7 μM
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