|N-(3-(((2-羟基萘-1-基)亚甲基)氨基)苯基)-2-苯基丙酰胺|CsnPharm

CAS No.: 1105698-15-4

N-(3-(((2-Hydroxynaphthalen-1-yl)methylene)amino)phenyl)-2-phenylpropanamide Catalog No. CSN18937

Synonyms: Salermide

Salermide, a reverse amide, can act as an inhibitor of sirt, especially of sirt2, with the property of inducing apoptosis of tumor cells.

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实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Mice: 30 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[2] (i.p.)
给药途径	i.p.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5351 mL
- 12.6754 mL
- 25.3508 mL
- 5 mM
- 0.5070 mL
- 2.5351 mL
- 5.0702 mL
- 10 mM
- 0.2535 mL
- 1.2675 mL
- 2.5351 mL

技术信息

CAS号

1105698-15-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H22N2O2

运输

蓝冰

分子量

394.47

别名

Salermide

溶解度

DMSO	100.0 mg/mL (253.5 mM)
Water	insoluble

动物实验配方

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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	23189967
MCF7 cells	30 μM	Proliferation assay	24-72 h	Antiproliferative activity against human MCF7 cells at 30 uM after 24 to 72 hrs	24340169
MDA-MB-231 cells	25 μM	Proliferation assay	24-72 h	Antiproliferative activity against human MDA-MB-231 cells at 25 uM after 24 to 72 hrs by MTT assay	23189967
MOLT4 cells	25 μM	Proliferation assay	24-72 h	Antiproliferative activity against human MOLT4 cells at 25 uM after 24 to 72 hrs by MTT assay	23189967
RKO cells	25 μM	Proliferation assay	24-72 h	Antiproliferative activity against human RKO cells at 25 uM after 24 to 72 hrs by MTT assay	23189967
U937 cells	50 μM	Function assay	45 h	Induction of apoptosis in human U937 cells at 50 uM after 45 hrs by flow cytometry	23189967

N-(3-(((2-Hydroxynaphthalen-1-yl)methylene)amino)phenyl)-2-phenylpropanamide Catalog No. CSN18937

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