Selisistat | EX-527 | CAS#49843-98-3 | SirT1 inhibitor

MedKoo Cat#: 319734 | Name: Selisistat

Description:

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

Selisistat, also known as EX-527, is a SirT1 inhibitor for treatment of Huntington's disease. Selisistat is widely used as a major inhibitor of Sirtuin enzymes, which are a family of highly conserved protein deacetylases and have been linked with caloric restriction and aging by modulating energy metabolism, genomic stability, and stress resistance.

Chemical Structure

Selisistat

CAS#49843-98-3

Theoretical Analysis

MedKoo Cat#: 319734

Name: Selisistat

CAS#: 49843-98-3

Chemical Formula: C13H13ClN2O

Exact Mass: 248.0716

Molecular Weight: 248.71

Elemental Analysis: C, 62.78; H, 5.27; Cl, 14.25; N, 11.26; O, 6.43

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 850.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 3,250.00	2 Weeks
2g	USD 4,650.00	2 Weeks

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Related CAS #

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Synonym

EX-527; EX-527; EX-527; Selisistat.

IUPAC/Chemical Name

6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

InChi Key

FUZYTVDVLBBXDL-UHFFFAOYSA-N

InChi Code

InChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)

SMILES Code

O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N

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

Soluble in DMSO, not in water

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:

Selisistat is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Galectin-9 in combination with Selisistat prolongs the survival of cardiac allografts in mice after cardiac transplantation. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease.

In vitro activity:

Selisitat suppressed hepatitis B replication by silencing the expression of SIRT1, therefore inhibiting its activity. Reference: Acta Virol. 2023;67(1):51-58. https://pubmed.ncbi.nlm.nih.gov/36950885/

In vivo activity:

Selisistat prevented the progression of high-fat diet-induced hepatic steatosis and fibrosis in Zucker rats, making it a promising candidate HFD-induced liver fibrosis inhibition. Selisistat reduced the serum levels of triglyceride, total cholesterol, alanine aminotransferase, and aspartate aminotransferase, and attenuated hepatic fibrosis. Selisistat upregulated SIRT2, SIRT3, and SIRT4 expression in the liver of HFD fed rats but downregulated TGF-β1 and α-SMA expression. It decreased proinflammatory cytokine production and hydroxyproline levels in the serum and SMAD4 expression and restored apoptotic protein expression. Reference: Cells. 2020 Apr 29;9(5):1101. https://pubmed.ncbi.nlm.nih.gov/32365537/

	Solvent	mg/mL	mM
Solubility
	DMSO	18.7	75.00
	Ethanol	12.4	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 248.71 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. Zhang W, Cui J, Li L, Chai L, Hou Q, Yu H. Notoginsenoside R1 inhibits hepatitis B virus replication by modulating SIRT1 activity. Acta Virol. 2023;67(1):51-58. doi: 10.4149/av_2023_105. PMID: 36950885. 2. Kundu A, Dey P, Park JH, Kim IS, Kwack SJ, Kim HS. EX-527 Prevents the Progression of High-Fat Diet-Induced Hepatic Steatosis and Fibrosis by Upregulating SIRT4 in Zucker Rats. Cells. 2020 Apr 29;9(5):1101. doi: 10.3390/cells9051101. PMID: 32365537; PMCID: PMC7290750. 3. Nikseresht S, Khodagholi F, Ahmadiani A. Protective effects of ex-527 on cerebral ischemia-reperfusion injury through necroptosis signaling pathway attenuation. J Cell Physiol. 2019 Feb;234(2):1816-1826. doi: 10.1002/jcp.27055. Epub 2018 Aug 1. PMID: 30067864.

In vitro protocol:

In vivo protocol:

1. Kundu A, Dey P, Park JH, Kim IS, Kwack SJ, Kim HS. EX-527 Prevents the Progression of High-Fat Diet-Induced Hepatic Steatosis and Fibrosis by Upregulating SIRT4 in Zucker Rats. Cells. 2020 Apr 29;9(5):1101. doi: 10.3390/cells9051101. PMID: 32365537; PMCID: PMC7290750. 2. Nikseresht S, Khodagholi F, Ahmadiani A. Protective effects of ex-527 on cerebral ischemia-reperfusion injury through necroptosis signaling pathway attenuation. J Cell Physiol. 2019 Feb;234(2):1816-1826. doi: 10.1002/jcp.27055. Epub 2018 Aug 1. PMID: 30067864.

1: Guo R, Wei Y, Du Y, Liu L, Zhang H, Ren R, Sun R, Zhang T, Xiong X, Zhao L, Wang H, Guo X, Zhu X. EX527, a sirtuins 1 inhibitor, sensitizes T-cell leukemia to death receptor-mediated apoptosis by downregulating cellular FLICE inhibitory protein. Cancer Biol Ther. 2024 Dec 31;25(1):2402588. doi: 10.1080/15384047.2024.2402588. Epub 2024 Sep 17. PMID: 39286953; PMCID: PMC11409494. 2: Duan H, Wang F, Wang K, Yang S, Zhang R, Xue C, Zhang L, Ma X, Du X, Kang J, Zhang Y, Zhao X, Hu J, Xiao L. Quercetin ameliorates oxidative stress-induced apoptosis of granulosa cells in dairy cow follicular cysts by activating autophagy via the SIRT1/ROS/AMPK signaling pathway. J Anim Sci Biotechnol. 2024 Sep 5;15(1):119. doi: 10.1186/s40104-024-01078-5. PMID: 39232832; PMCID: PMC11375867. 3: Lu F, Wang R, Cheng Y, Li X. Preconditioning with β-hydroxybutyrate attenuates lung ischemia-reperfusion injury by suppressing alveolar macrophage pyroptosis through the SIRT1-FOXO3 signaling pathway. FASEB J. 2024 Sep 15;38(17):e70027. doi: 10.1096/fj.202401188R. PMID: 39221615. 4: Yadav V, Pandey V, Gaglani P, Srivastava A, Soni, Subhashini. Inhibiting SIRT-2 by AK-7 restrains airway inflammation and oxidative damage promoting lung resurgence through NF-kB and MAP kinase signaling pathway. Front Immunol. 2024 Jun 24;15:1404122. doi: 10.3389/fimmu.2024.1404122. PMID: 38979411; PMCID: PMC11228164. 5: Zhao M, Qiu D, Miao X, Yang W, Li S, Cheng X, Tang J, Chen H, Ruan H, Liu Y, Wei C, Xiao J. Melatonin Delays Arthritis Inflammation and Reduces Cartilage Matrix Degradation through the SIRT1-Mediated NF-κB/Nrf2/TGF-β/BMPs Pathway. Int J Mol Sci. 2024 Jun 4;25(11):6202. doi: 10.3390/ijms25116202. PMID: 38892389; PMCID: PMC11172638. 6: Liao X, Lu J, Huang Z, Lin J, Zhang M, Chen H, Lin X, Gao X, Gong S. Aminophylline suppresses chronic renal failure progression by activating SIRT1/AMPK/mTOR-dependent autophagy. Acta Biochim Biophys Sin (Shanghai). 2024 May 29. doi: 10.3724/abbs.2024049. Epub ahead of print. PMID: 38808395. 7: Zhao X, Li M, Lu Y, Wang M, Xiao J, Xie Q, He X, Shuai S. Sirt1 inhibits macrophage polarization and inflammation in gouty arthritis by inhibiting the MAPK/NF-κB/AP-1 pathway and activating the Nrf2/HO-1 pathway. Inflamm Res. 2024 Jul;73(7):1173-1184. doi: 10.1007/s00011-024-01890-9. Epub 2024 May 13. PMID: 38739197; PMCID: PMC11214610. 8: Zylberberg B, Poodts M, Roncoroni J, Coronel MF, Mazzone GL. Resveratrol evokes neuroprotective effects and improves foot stance following kainate- induced excitotoxic damage to the mouse spinal cord. Neuropharmacology. 2024 Jun 1;250:109906. doi: 10.1016/j.neuropharm.2024.109906. Epub 2024 Mar 16. PMID: 38494123. 9: Bai J, Wang X, Chen Y, Yuan Q, Yang Z, Mi Y, Zhang C. Nobiletin Ameliorates Aging of Chicken Ovarian Prehierarchical Follicles by Suppressing Oxidative Stress and Promoting Autophagy. Cells. 2024 Feb 27;13(5):415. doi: 10.3390/cells13050415. PMID: 38474379; PMCID: PMC10930417. 10: Shu MQ, Dai YY, Song LJ, Ma D, Liu KX, Miao ZY, Wei RH, Yin JZ, Ma CG, Huang JJ. [Tetramethylpyrazine regulates angiogenesis of endothelial cells in cerebral ischemic stroke injury via SIRT1/VEGFA signaling pathway]. Zhongguo Zhong Yao Za Zhi. 2024 Jan;49(1):162-174. Chinese. doi: 10.19540/j.cnki.cjcmm.20231116.303. PMID: 38403349. 11: Cheng Y, Huang P, Zou Q, Tian H, Cheng Q, Ding H. Nicotinamide mononucleotide alleviates seizures via modulating SIRT1-PGC-1α mediated mitochondrial fusion and fission. J Neurochem. 2024 Jan 9. doi: 10.1111/jnc.16041. Epub ahead of print. PMID: 38194959. 12: Wang J, Zhao P, Cheng P, Zhang Z, Yang S, Wang J, Wang X, Zhu G. Exploring the effect of Anshen Dingzhi prescription on hippocampal mitochondrial signals in single prolonged stress mouse model. J Ethnopharmacol. 2024 Apr 6;323:117713. doi: 10.1016/j.jep.2024.117713. Epub 2024 Jan 3. PMID: 38181935. 13: Zheng Y, Shao N, Yang X, Shi Y, Xu G. Resveratrol ameliorates intestinal lipid metabolism through the PPAR signaling pathway in high-fat diet-fed red tilapia (Oreochromis niloticus). Fish Shellfish Immunol. 2024 Feb;145:109302. doi: 10.1016/j.fsi.2023.109302. Epub 2023 Dec 20. PMID: 38128680. 14: Zhang J, Zhu Q, Peng Z, Li XJ, Ding PF, Gao S, Sheng B, Liu Y, Lu Y, Zhuang Z, Hang CH, Li W. Menaquinone-4 attenuates ferroptosis by upregulating DHODH through activation of SIRT1 after subarachnoid hemorrhage. Free Radic Biol Med. 2024 Jan;210:416-429. doi: 10.1016/j.freeradbiomed.2023.11.031. Epub 2023 Nov 30. Erratum in: Free Radic Biol Med. 2024 Jul;219:180-183. doi: 10.1016/j.freeradbiomed.2024.04.227. PMID: 38042225. 15: Chen XM, Guo YJ, Ling HW, Zeng R. The Effect of Resveratrol in Sirt1/CST Pathway to Inhibit TNF-α Induced Inflammatory Response in Rat Primary Fibroblast-Like Synoviocytes. Biol Pharm Bull. 2023;46(11):1592-1600. doi: 10.1248/bpb.b23-00401. PMID: 37914362. 16: Lo Cigno I, Calati F, Girone C, Borgogna C, Venuti A, Boldorini R, Gariglio M. SIRT1 is an actionable target to restore p53 function in HPV-associated cancer therapy. Br J Cancer. 2023 Nov;129(11):1863-1874. doi: 10.1038/s41416-023-02465-x. Epub 2023 Oct 14. PMID: 37838812; PMCID: PMC10667542. 17: Tang Q, Meng C, Liu Y, Cheng Y, Liu Y, Long Y, Sun S, Feng F. Silencing SIRT1 promotes the anti-HBV action of IFN-α by regulating Pol expression and activating the JAK-STAT signaling pathway. Int Immunopharmacol. 2023 Nov;124(Pt B):110939. doi: 10.1016/j.intimp.2023.110939. Epub 2023 Sep 21. PMID: 37741128. 18: Cao P, Wang Y, Zhang C, Sullivan MA, Chen W, Jing X, Yu H, Li F, Wang Q, Zhou Z, Wang Q, Tian W, Qiu Z, Luo L. Quercetin ameliorates nonalcoholic fatty liver disease (NAFLD) via the promotion of AMPK-mediated hepatic mitophagy. J Nutr Biochem. 2023 Oct;120:109414. doi: 10.1016/j.jnutbio.2023.109414. Epub 2023 Jul 7. PMID: 37423322. 19: Liang SP, Wang XZ, Piao MH, Chen X, Wang ZC, Li C, Wang YB, Lu S, He C, Wang YL, Chi GF, Ge PF. Activated SIRT1 contributes to DPT-induced glioma cell parthanatos by upregulation of NOX2 and NAT10. Acta Pharmacol Sin. 2023 Oct;44(10):2125-2138. doi: 10.1038/s41401-023-01109-3. Epub 2023 Jun 5. PMID: 37277492; PMCID: PMC10545831. 20: Monte-Serrano E, Morejón-García P, Campillo-Marcos I, Campos-Díaz A, Navarro-Carrasco E, Lazo PA. The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase. Epigenetics Chromatin. 2023 May 13;16(1):18. doi: 10.1186/s13072-023-00494-7. PMID: 37179361; PMCID: PMC10182654.