Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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E129892-5mg | 5mg | In stock | $53.90 | |
E129892-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
E129892-25mg | 25mg | In stock | $118.90 | |
E129892-50mg | 50mg | In stock | $187.90 | |
E129892-100mg | 100mg | In stock | $296.90 | |
E129892-250mg | 250mg | In stock | $668.90 |
Selective SIRT1 Inhibitor
Synonyms | EX-527 (SELISISTAT) | SEN0014196 | SEN-0014196 | AB88646 | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide | FT-0698480 | SELISISTAT [WHO-DD] | SCHEMBL1275557 | 1H-Carbazole-1-carboxamide, 6-chloro-2,3,4,9-tetrahydro- | EX 527 | HMS3426E09 | 6-Chlo |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | EX 527 is a potent and selective inhibitor of the SIRT1 class III histone deacetylase enzyme, thought to block the release of deacetylated peptide and O-acetyl-ADP-ribose from the enzyme following the deacetylation process. EX 527 has been used a powerful |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of sirtuin 1 |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | EX 527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits >200-fold selectivity against SIRT2 and SIRT3. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide |
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INCHI | 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) |
InChi Key | FUZYTVDVLBBXDL-UHFFFAOYSA-N |
Canonical SMILES | C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N |
Isomeric SMILES | C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N |
WGK Germany | 3 |
PubChem CID | 5113032 |
Molecular Weight | 248.71 |
PubChem CID | 5113032 |
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CAS Registry No. | 49843-98-3 |
ChEMBL Ligand | CHEMBL420311 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
K2230583 | Certificate of Analysis | Sep 12, 2024 | E129892 |
K2230599 | Certificate of Analysis | Sep 12, 2024 | E129892 |
K2230667 | Certificate of Analysis | Sep 12, 2024 | E129892 |
K2230708 | Certificate of Analysis | Sep 12, 2024 | E129892 |
K2230732 | Certificate of Analysis | Sep 12, 2024 | E129892 |
K2230738 | Certificate of Analysis | Sep 12, 2024 | E129892 |
A1527018 | Certificate of Analysis | Jun 13, 2024 | E129892 |
Solubility | Soluble in DMSO (10 mg/ml), ethanol (5 mg/ml), DMF (~20 mg/ml), and DMSO:PBS (1:1 pH 7.2) (~0.5 mg/ml). |
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Sensitivity | Heat Sensitive |
Refractive Index | 1.69 |
Boil Point(°C) | 531.72°C/760mmHg |
Melt Point(°C) | 178°C |
Pictogram(s) | GHS06, GHS07 |
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Signal | Danger |
Hazard Statements | H319:Causes serious eye irritation H301:Toxic if swallowed |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P337+P317:If eye irritation persists: Get medical help. |
WGK Germany | 3 |
1. Xiu Yanghui, Su Yu, Gao Lihua, Yuan Hui, Xu Sennan, Liu Ying, Qiu Yan, Liu Zhen, Li Yuhang. (2023) Corylin accelerated wound healing through SIRT1 and PI3K/AKT signaling: a candidate remedy for chronic non-healing wounds. Frontiers in Pharmacology, 14 [PMID:37266148] [10.3389/fphar.2023.1153810] |
2. Bo Zou, Yue Fu, Chaofan Cao, Dianzhu Pan, Wei Wang, Lingfei Kong. (2021) Gentiopicroside ameliorates ovalbumin-induced airway inflammation in a mouse model of allergic asthma via regulating SIRT1/NF-κB signaling pathway. PULMONARY PHARMACOLOGY & THERAPEUTICS, 68 (102034). [PMID:33887491] [10.1016/j.pupt.2021.102034] |
3. Jun Huang, Xue Wang, Yi Zhu, Zhe Li, Yu-Ting Zhu, Jun-Chao Wu, Zheng-Hong Qin, Min Xiang, Fang Lin. (2019) Exercise activates lysosomal function in the brain through AMPK-SIRT1-TFEB pathway. CNS Neuroscience & Therapeutics, 25 (6): (796-807). [PMID:30864262] [10.1111/cns.13114] |
4. Qiao Lin, Xiu-Ying Chen, Ji Zhang, Yong-Liang Yuan, Wen Zhao, Bo Wei. (2018) Upregulation of SIRT1 contributes to the cardioprotective effect of Rutin against myocardial ischemia-reperfusion injury in rats. Journal of Functional Foods, 46 (227). [PMID:] [10.1016/j.jff.2018.05.007] |
1. Blander G, Guarente L. (2004) The Sir2 family of protein deacetylases.. Annu Rev Biochem, 73 (13): (417-35). [PMID:15189148] [10.1021/op500134e] |
2. Solomon JM, Pasupuleti R, Xu L, McDonagh T, Curtis R, DiStefano PS, Huber LJ. (2006) Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage.. Mol Cell Biol, 26 (1): (28-38). [PMID:16354677] [10.1021/op500134e] |
3. Broussy S, Laaroussi H, Vidal M. (2020) Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat).. J Enzyme Inhib Med Chem, 35 (1): (1124-1136). [PMID:32366137] [10.1021/op500134e] |
4. Zhan H et al.. (2021) Downregulation of miR-128 Ameliorates Ang II-Induced Cardiac Remodeling via SIRT1/PIK3R1 Multiple Targets.. Oxid Med Cell Longev, 2021 (8889195). [PMID:34646427] |
5. Mao H et al.. (2022) Fucoxanthin Attenuates Oxidative Damage by Activating the Sirt1/Nrf2/HO-1 Signaling Pathway to Protect the Kidney from Ischemia-Reperfusion Injury.. Oxid Med Cell Longev, 2022 (7444430). [PMID:35126819] |
6. Chen J et al.. (2021) Melatonin attenuates prostatic inflammation and pelvic pain via Sirt1-dependent inhibition of the NLRP3 inflammasome in an EAP mouse model.. Prostate, 81 (15): (1179-1190). [PMID:34418127] |
7. Zhang J et al.. (2020) N1-Methylnicotinamide Improves Hepatic Insulin Sensitivity via Activation of SIRT1 and Inhibition of FOXO1 Acetylation.. J Diabetes Res, 2020 (1080152). [PMID:32280711] |
8. Ruan C et al.. (2021) Neuroprotective effects of metformin on cerebral ischemia-reperfusion injury by regulating PI3K/Akt pathway.. Brain Behav, 11 (10): (e2335). [PMID:34473417] |
9. Zhang J et al.. (2022) Resveratrol inhibits hepatic stellate cell activation by regulating autophagy and apoptosis through the SIRT1 and JNK signaling pathways.. J Food Biochem, 46 (12): (e14463). [PMID:36314441] |
10. Liu SP et al.. (2019) Secukinumab attenuates reactive astrogliosis via IL-17RA/(C/EBPß)/SIRT1 pathway in a rat model of germinal matrix hemorrhage.. CNS Neurosci Ther, [PMID:31020769] |
11. Wu Y et al.. (2020) Suppression of sirtuin 1 alleviates airway inflammation through mTOR-mediated autophagy.. Mol Med Rep, 22 (3): (2219-2226). [PMID:32705226] |
12. Xiu Yanghui, Su Yu, Gao Lihua, Yuan Hui, Xu Sennan, Liu Ying, Qiu Yan, Liu Zhen, Li Yuhang. (2023) Corylin accelerated wound healing through SIRT1 and PI3K/AKT signaling: a candidate remedy for chronic non-healing wounds. Frontiers in Pharmacology, 14 [PMID:37266148] [10.3389/fphar.2023.1153810] |
13. Bo Zou, Yue Fu, Chaofan Cao, Dianzhu Pan, Wei Wang, Lingfei Kong. (2021) Gentiopicroside ameliorates ovalbumin-induced airway inflammation in a mouse model of allergic asthma via regulating SIRT1/NF-κB signaling pathway. PULMONARY PHARMACOLOGY & THERAPEUTICS, 68 (102034). [PMID:33887491] [10.1016/j.pupt.2021.102034] |
14. Jun Huang, Xue Wang, Yi Zhu, Zhe Li, Yu-Ting Zhu, Jun-Chao Wu, Zheng-Hong Qin, Min Xiang, Fang Lin. (2019) Exercise activates lysosomal function in the brain through AMPK-SIRT1-TFEB pathway. CNS Neuroscience & Therapeutics, 25 (6): (796-807). [PMID:30864262] [10.1111/cns.13114] |
15. Qiao Lin, Xiu-Ying Chen, Ji Zhang, Yong-Liang Yuan, Wen Zhao, Bo Wei. (2018) Upregulation of SIRT1 contributes to the cardioprotective effect of Rutin against myocardial ischemia-reperfusion injury in rats. Journal of Functional Foods, 46 (227). [PMID:] [10.1016/j.jff.2018.05.007] |