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Salermide

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Chemical Structure| 1105698-15-4 同义名 : -
CAS号 : 1105698-15-4
货号 : A557147
分子式 : C26H22N2O2
纯度 : 98%
分子量 : 394.465
MDL号 : MFCD12912446
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(126.75 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • SIRT1
描述 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].
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
参考文献

[1]Lara E, Mai A, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91.

[2]Lara E, Mai A, Calvanese V, Altucci L, Lopez-Nieva P, Martinez-Chantar ML, Varela-Rey M, Rotili D, Nebbioso A, Ropero S, Montoya G, Oyarzabal J, Velasco S, Serrano M, Witt M, Villar-Garea A, Imhof A, Mato JM, Esteller M, Fraga MF. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91. doi: 10.1038/onc.2008.436. Epub 2008 Dec 8. Erratum in: Oncogene. 2009 Feb 26;28(8):1168. Inhof, A [corrected to Imhof, A]. PMID: 19060927.