Salermide

Modify Date: 2024-01-02 13:38:41

Salermide Structure
Salermide structure
Common Name Salermide
CAS Number 1105698-15-4 Molecular Weight 394.465
Density 1.2±0.1 g/cm3 Boiling Point 666.7±50.0 °C at 760 mmHg
Molecular Formula C26H22N2O2 Melting Point N/A
MSDS Chinese USA Flash Point 357.0±30.1 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of Salermide


Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.

 Names

Name N-[3-[(2-oxonaphthalen-1-ylidene)methylamino]phenyl]-2-phenylpropanamide
Synonym More Synonyms

 Salermide Biological Activity

Description Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
Related Catalog
Target

SIRT1

SIRT2

In Vitro Salermide shows a dose-dependent inhibition that rises to 80% at 90 μM and 25 μM against Sirt1 and Sirt2, respectively. Salermide can prompt tumour-specific cell death in a wide range of human cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231). Incubation with 100 μM Salermide alone resulted in an increase of cytosolicactivated caspase 3 and a decrease of mitochondrialcytochrome. Salermide alone can induce apoptosis through both extrinsic and intrinsic pathways. Salermide had several antitumorigenic advantages over the earlier described class III HDAC inhibitors: firstly, it mimics the universal proapoptotic effect on cancer samples exhibited by the classical class I, II and IV HDAC inhibitors, and secondly, its proapoptotic effect is cancer-specific[1].
In Vivo Salermide is well tolerated by mice at concentrations up to 100 μM. Salermide's mechanism of action in vivo is specifically mediated by Sirt1. Intraperitoneal feeding of Salermide has no apparent toxicity in nude mice[1].
Cell Assay Cell lines (SW480, MDA-MB-231, MOLT4, KG1A, K562 and Raji) are used in the study. Cell viability is determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. IC50 index is calculated using four Salermide concentrations (25, 50, 75 and 100 μM) for 24 h. The percentage of apoptotic cells is determined with the FACSCalibur apparatus[1].
Animal Admin Mice: To assess possible adverse effects of Salermide in vivo. To do this, a group of 10 nude mice are intraperitoneal injected 100 μL of 100 μM of Salermide to over 34 days. Diet consumption, body-weight gain, and postural and behavioural changes are monitored throughout the study[1].
References

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

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 666.7±50.0 °C at 760 mmHg
Molecular Formula C26H22N2O2
Molecular Weight 394.465
Flash Point 357.0±30.1 °C
Exact Mass 394.168121
PSA 61.69000
LogP 5.40
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.623
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H317-H412
Precautionary Statements P273-P280
RIDADR NONH for all modes of transport

 Synthetic Route

~86%

Salermide Structure

Salermide

CAS#:1105698-15-4

Literature: Rotili, Dante; Tarantino, Domenico; Nebbioso, Angela; Paolini, Chantal; Huidobro, Covadonga; Lara, Ester; Mellini, Paolo; Lenoci, Alessia; Pezzi, Riccardo; Botta, Giorgia; Lahtela-Kakkonen, Maija; Poso, Antti; Steinkuehler, Christian; Gallinari, Paola; De Maria, Ruggero; Fraga, Mario; Esteller, Manel; Altucci, Lucia; Mai, Antonello Journal of Medicinal Chemistry, 2012 , vol. 55, # 24 p. 10937 - 10947

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Salermide Structure

Salermide

CAS#:1105698-15-4

Literature: Rotili, Dante; Tarantino, Domenico; Nebbioso, Angela; Paolini, Chantal; Huidobro, Covadonga; Lara, Ester; Mellini, Paolo; Lenoci, Alessia; Pezzi, Riccardo; Botta, Giorgia; Lahtela-Kakkonen, Maija; Poso, Antti; Steinkuehler, Christian; Gallinari, Paola; De Maria, Ruggero; Fraga, Mario; Esteller, Manel; Altucci, Lucia; Mai, Antonello Journal of Medicinal Chemistry, 2012 , vol. 55, # 24 p. 10937 - 10947

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 Synonyms

N-(3-{(E)-[(2-Hydroxy-1-naphthyl)methylene]amino}phenyl)-2-phenylpropanamide
Salermide
Benzeneacetamide, N-[3-[[(1E)-(2-hydroxy-1-naphthalenyl)methylene]amino]phenyl]-α-methyl-
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