Salermide | CAS#1105698-15-4 | Sirtuin inhibitor

MedKoo Cat#: 407409 | Name: Salermide

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Salermide is a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Salermide was well tolerated by mice at concentrations up to 100 muM and prompted tumour-specific cell death in a wide range of human cancer cell lines. The antitumour activity of Salermide was primarily because of a massive induction of apoptosis. Salermide up-regulates death receptor 5 expression through the ATF4-ATF3-CHOP axis and leads to apoptosis in human cancer cells.

Chemical Structure

Salermide

CAS#1105698-15-4

Theoretical Analysis

MedKoo Cat#: 407409

Name: Salermide

CAS#: 1105698-15-4

Chemical Formula: C26H22N2O2

Exact Mass: 394.1681

Molecular Weight: 394.47

Elemental Analysis: C, 79.17; H, 5.62; N, 7.10; O, 8.11

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 550.00	2 Weeks
50mg	USD 1,050.00	2 Weeks
100mg	USD 1,500.00	2 Weeks

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Synonym

Salermide

IUPAC/Chemical Name

N-[3-[[(2-hydroxy-1-naphthalenyl)methylene]amino]phenyl]-a-methyl-benzeneacetamide

InChi Key

HQSSEGBEYORUBY-WPWMEQJKSA-N

InChi Code

InChI=1S/C26H22N2O2/c1-18(19-8-3-2-4-9-19)26(30)28-22-12-7-11-21(16-22)27-17-24-23-13-6-5-10-20(23)14-15-25(24)29/h2-18,29H,1H3,(H,28,30)/b27-17+

SMILES Code

O=C(NC1=CC=CC(/N=C/C2=C3C=CC=CC3=CC=C2O)=C1)C(C)C4=CC=CC=C4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Salermide is an inhibitor of SIRT1 and SIRT2, causing tumor-specific apoptotic cell death.

In vitro activity:

This study investigated the effects of HDAC inhibitors, including Salermide, on human pancreatic cancer cells (BxPC-3) alone and in combination with EF24 (EF). Salermide has potential in impacting pancreatic cancer cell behavior. Salermide significantly reduced the viability of BxPC-3 cells. Salermide and MS-275 treatments increased the acetylation of histone H3 and H4 and caused cell cycle arrest at the G1 phase. Reference: EXCLI J. 2016 Apr 4;15:246-55. https://pubmed.ncbi.nlm.nih.gov/27330528/

In vivo activity:

This study demonstrates that the combination of oxamflatin and salermide ameliorated duchenne muscular dystrophy mutant zebrafish skeletal muscle degeneration. The combination caused increased levels of histone H4 acetylation in zebrafish larvae. Reference: Skelet Muscle. 2020 Oct 15;10(1):29. https://pubmed.ncbi.nlm.nih.gov/33059738/

Preparing Stock Solutions

The following data is based on the product molecular weight 394.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yar Saglam AS, Yilmaz A, Onen HI, Alp E, Kayhan H, Ekmekci A. HDAC inhibitors, MS-275 and salermide, potentiates the anticancer effect of EF24 in human pancreatic cancer cells. EXCLI J. 2016 Apr 4;15:246-55. doi: 10.17179/excli2016-186. PMID: 27330528; PMCID: PMC4908665. 2. Dastjerdi MN, Salahshoor MR, Mardani M, Rabbani M, Hashemibeni B, Gharagozloo M, Kazemi M, Esmaeil N, Roshankhah Sh, Golmohammadi R, Mobarakian M. The apoptotic effects of sirtuin1 inhibitor on the MCF-7 and MRC-5 cell lines. Res Pharm Sci. 2013 Apr;8(2):79-89. PMID: 24019817; PMCID: PMC3764679. 3. Farr GH 3rd, Morris M, Gomez A, Pham T, Kilroy E, Parker EU, Said S, Henry C, Maves L. A novel chemical-combination screen in zebrafish identifies epigenetic small molecule candidates for the treatment of Duchenne muscular dystrophy. Skelet Muscle. 2020 Oct 15;10(1):29. doi: 10.1186/s13395-020-00251-4. PMID: 33059738; PMCID: PMC7559456. 4. 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.

In vitro protocol:

In vivo protocol:

1. Farr GH 3rd, Morris M, Gomez A, Pham T, Kilroy E, Parker EU, Said S, Henry C, Maves L. A novel chemical-combination screen in zebrafish identifies epigenetic small molecule candidates for the treatment of Duchenne muscular dystrophy. Skelet Muscle. 2020 Oct 15;10(1):29. doi: 10.1186/s13395-020-00251-4. PMID: 33059738; PMCID: PMC7559456. 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.

1: Wen Z, Ablimit A. Comprehensive analysis of scRNA-Seq and bulk RNA-Seq reveals ubiquitin promotes pulmonary fibrosis in chronic pulmonary diseases. Sci Rep. 2024 Sep 11;14(1):21195. doi: 10.1038/s41598-024-70659-1. PMID: 39261509; PMCID: PMC11390722. 2: Alkhatabi HA. Deciphering aging-associated molecular mechanisms in bone marrow derived hematopoietic stem cells in the elderly using NGS data. Bioinformation. 2024 Feb 29;20(2):180-189. doi: 10.6026/973206300200180. PMID: 38497076; PMCID: PMC10941783. 3: Hasegawa EH, Farr GH 3rd, Maves L. Comparison of Pronase versus Manual Dechorionation of Zebrafish Embryos for Small Molecule Treatments. J Dev Biol. 2023 Mar 28;11(2):16. doi: 10.3390/jdb11020016. PMID: 37092478; PMCID: PMC10123619. 4: Eid M, Dzreyan V, Demyanenko S. Sirtuins 1 and 2 in the Acute Period After Photothrombotic Stroke: Expression, Localization and Involvement in Apoptosis. Front Physiol. 2022 Apr 27;13:782684. doi: 10.3389/fphys.2022.782684. PMID: 35574497; PMCID: PMC9092253. 5: Keskin-Aktan A, Akbulut KG, Abdi S, Akbulut H. SIRT2 and FOXO3a expressions in the cerebral cortex and hippocampus of young and aged male rats: antioxidant and anti-apoptotic effects of melatonin. Biol Futur. 2022 Mar;73(1):71-85. doi: 10.1007/s42977-021-00102-3. Epub 2021 Oct 27. PMID: 34708398. 6: Harris MB, Hoffman RM, Olesiak M. Chronic Exercise Mitigates the Effects of Sirtuin Inhibition by Salermide on Endothelium-Dependent Vasodilation. Cardiovasc Toxicol. 2021 Oct;21(10):790-799. doi: 10.1007/s12012-021-09669-8. Epub 2021 Jun 29. PMID: 34185244. 7: Chen M, Chen Z, Huang D, Sun C, Xie J, Chen T, Zhao X, Huang Y, Li D, Wu B, Wu D. Myricetin inhibits TNF-α-induced inflammation in A549 cells via the SIRT1/NF-κB pathway. Pulm Pharmacol Ther. 2020 Dec;65:102000. doi: 10.1016/j.pupt.2021.102000. Epub 2021 Feb 16. Erratum in: Pulm Pharmacol Ther. 2021 Jun;68:102031. doi: 10.1016/j.pupt.2021.102031. PMID: 33601000. 8: Farr GH 3rd, Morris M, Gomez A, Pham T, Kilroy E, Parker EU, Said S, Henry C, Maves L. A novel chemical-combination screen in zebrafish identifies epigenetic small molecule candidates for the treatment of Duchenne muscular dystrophy. Skelet Muscle. 2020 Oct 15;10(1):29. doi: 10.1186/s13395-020-00251-4. PMID: 33059738; PMCID: PMC7559456. 9: Joo SY, Aung JM, Shin M, Moon EK, Kong HH, Goo YK, Chung DI, Hong Y. The role of the Acanthamoeba castellanii Sir2-like protein in the growth and encystation of Acanthamoeba. Parasit Vectors. 2020 Jul 22;13(1):368. doi: 10.1186/s13071-020-04237-5. PMID: 32698828; PMCID: PMC7376869. 10: Guo Q, Chen S, Rao X, Li Y, Pan M, Fu G, Yao Y, Gao X, Tang P, Zhou Y, Xu X, Gao J, Hua G. Inhibition of SIRT1 promotes taste bud stem cell survival and mitigates radiation-induced oral mucositis in mice. Am J Transl Res. 2019 Aug 15;11(8):4789-4799. PMID: 31497199; PMCID: PMC6731402. 11: Mu N, Lei Y, Wang Y, Wang Y, Duan Q, Ma G, Liu X, Su L. Inhibition of SIRT1/2 upregulates HSPA5 acetylation and induces pro-survival autophagy via ATF4-DDIT4-mTORC1 axis in human lung cancer cells. Apoptosis. 2019 Oct;24(9-10):798-811. doi: 10.1007/s10495-019-01559-3. PMID: 31321634. 12: De U, Son JY, Sachan R, Park YJ, Kang D, Yoon K, Lee BM, Kim IS, Moon HR, Kim HS. A New Synthetic Histone Deacetylase Inhibitor, MHY2256, Induces Apoptosis and Autophagy Cell Death in Endometrial Cancer Cells via p53 Acetylation. Int J Mol Sci. 2018 Sep 13;19(9):2743. doi: 10.3390/ijms19092743. PMID: 30217020; PMCID: PMC6164480. 13: Keskin-Aktan A, Akbulut KG, Yazici-Mutlu Ç, Sonugur G, Ocal M, Akbulut H. The effects of melatonin and curcumin on the expression of SIRT2, Bcl-2 and Bax in the hippocampus of adult rats. Brain Res Bull. 2018 Mar;137:306-310. doi: 10.1016/j.brainresbull.2018.01.006. Epub 2018 Jan 8. PMID: 29325994. 14: Tang L, Chen Q, Meng Z, Sun L, Zhu L, Liu J, Hu J, Ni Z, Wang X. Suppression of Sirtuin-1 Increases IL-6 Expression by Activation of the Akt Pathway During Allergic Asthma. Cell Physiol Biochem. 2017;43(5):1950-1960. doi: 10.1159/000484119. Epub 2017 Oct 20. PMID: 29055943. 15: Chen T, Dai SH, Li X, Luo P, Zhu J, Wang YH, Fei Z, Jiang XF. Sirt1-Sirt3 axis regulates human blood-brain barrier permeability in response to ischemia. Redox Biol. 2018 Apr;14:229-236. doi: 10.1016/j.redox.2017.09.016. Epub 2017 Sep 22. PMID: 28965081; PMCID: PMC5633840. 16: Park EY, Woo Y, Kim SJ, Kim DH, Lee EK, De U, Kim KS, Lee J, Jung JH, Ha KT, Choi WS, Kim IS, Lee BM, Yoon S, Moon HR, Kim HS. Anticancer Effects of a New SIRT Inhibitor, MHY2256, against Human Breast Cancer MCF-7 Cells via Regulation of MDM2-p53 Binding. Int J Biol Sci. 2016 Dec 6;12(12):1555-1567. doi: 10.7150/ijbs.13833. PMID: 27994519; PMCID: PMC5166496. 17: Yar Saglam AS, Yilmaz A, Onen HI, Alp E, Kayhan H, Ekmekci A. HDAC inhibitors, MS-275 and salermide, potentiates the anticancer effect of EF24 in human pancreatic cancer cells. EXCLI J. 2016 Apr 4;15:246-55. doi: 10.17179/excli2016-186. PMID: 27330528; PMCID: PMC4908665. 18: Singh R, Yadav BS, Singh S, Pandey PN, Mani A. In-silico screening of Schistosoma mansoni Sirtuin1 inhibitors for prioritization of drug candidates. Springerplus. 2016 Mar 7;5:286. doi: 10.1186/s40064-016-1891-4. PMID: 27066323; PMCID: PMC4781818. 19: Moretti NS, da Silva Augusto L, Clemente TM, Antunes RP, Yoshida N, Torrecilhas AC, Cano MI, Schenkman S. Characterization of Trypanosoma cruzi Sirtuins as Possible Drug Targets for Chagas Disease. Antimicrob Agents Chemother. 2015 Aug;59(8):4669-79. doi: 10.1128/AAC.04694-14. Epub 2015 May 26. PMID: 26014945; PMCID: PMC4505258. 20: Kim TH, Kim HS, Kang YJ, Yoon S, Lee J, Choi WS, Jung JH, Kim HS. Psammaplin A induces Sirtuin 1-dependent autophagic cell death in doxorubicin-resistant MCF-7/adr human breast cancer cells and xenografts. Biochim Biophys Acta. 2015 Feb;1850(2):401-10. doi: 10.1016/j.bbagen.2014.11.007. Epub 2014 Nov 12. PMID: 25445714.