Salermide |
Catalog No.GC14817 |
SIRT1 and SIRT2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1105698-15-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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 experiment: | 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. |
Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
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].
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].
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.
Cas No. | 1105698-15-4 | SDF | |
Chemical Name | (S,E)-N-(3-(((2-oxonaphthalen-1(2H)-ylidene)methyl)amino)phenyl)-2-phenylpropanamide | ||
Canonical SMILES | O=C([C@@H](C)C1=CC=CC=C1)NC2=CC=CC(N/C=C3C4=CC=CC=C4C=CC\3=O)=C2 | ||
Formula | C26H22N2O2 | M.Wt | 394.47 |
Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.535 mL | 12.6752 mL | 25.3505 mL |
5 mM | 0.507 mL | 2.535 mL | 5.0701 mL |
10 mM | 0.2535 mL | 1.2675 mL | 2.535 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 22 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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