EX 527 (Selisistat) - ≥98%, high purity , CAS No.49843-98-3, Inhibitor of sirtuin 1

Item Number
E129892
Grouped product items
SKUSizeAvailabilityPrice Qty
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

View related series
sirtuin 1 Inhibitor

Basic Description

SynonymsEX-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
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsEX 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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of sirtuin 1
NoteWherever 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.
A selective inhibitor of SIRT1 over SIRT2 and SIRT3

Associated Targets(Human)

SIRT2 Tchem NAD-dependent protein deacetylase sirtuin-2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIRT1 Tchem NAD-dependent protein deacetylase sirtuin-1 (26 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
YES1 Tclin Tyrosine-protein kinase YES (2781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HT-29 (80576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
K562 (73714 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF7 (126967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U-937 (7138 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
A549 (127892 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-116 (91556 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NCI-H460 (60772 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HUVEC (11049 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SIRT3 Tchem NAD-dependent deacetylase sirtuin 3 (1285 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SIRT2 Tchem NAD-dependent deacetylase sirtuin 2 (3979 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SIRT1 Tchem NAD-dependent deacetylase sirtuin 1 (3505 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hs 683 (377 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CD38 Tclin Lymphocyte differentiation antigen CD38 (364 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SIRT5 Tchem NAD-dependent protein deacylase sirtuin-5, mitochondrial (1056 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
UBE2T Tbio Ubiquitin-conjugating enzyme E2 T (35 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HD1 Histone deacetylase (38 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Ube2d3 Ubiquitin-conjugating enzyme E2 D3 (38 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
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

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

7 results found

Lot NumberCertificate TypeDateItem
K2230583Certificate of AnalysisSep 12, 2024 E129892
K2230599Certificate of AnalysisSep 12, 2024 E129892
K2230667Certificate of AnalysisSep 12, 2024 E129892
K2230708Certificate of AnalysisSep 12, 2024 E129892
K2230732Certificate of AnalysisSep 12, 2024 E129892
K2230738Certificate of AnalysisSep 12, 2024 E129892
A1527018Certificate of AnalysisJun 13, 2024 E129892

Chemical and Physical Properties

SolubilitySoluble 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).
SensitivityHeat Sensitive
Refractive Index1.69
Boil Point(°C)531.72°C/760mmHg
Melt Point(°C)178°C

Safety and Hazards(GHS)

Pictogram(s) GHS06,   GHS07
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

Related Documents

Citations of This Product

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]

References

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]

Solution Calculators