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

5 Citations COA COA
In stock
Item Number
E129892
Grouped product items
SKU Size
Availability
 Price Qty
E129892-5mg
5mg
3
$53.90
E129892-10mg
10mg
3
$64.90
E129892-25mg
25mg
3
$118.90
E129892-50mg
50mg
3
$187.90
E129892-100mg
100mg
3
$296.90
E129892-250mg
250mg
3
$668.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Selective SIRT1 Inhibitor

View related series
Cell Cycle (2830) Cell Cycle/DNA Damage (2602) Epigenetics (1496) Histone Modification (1379) Sirtuin (94) sirtuin 1 Inhibitor (3)

Basic Description

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
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
This product requires cold chain shipping. Ground and other economy services are not available.
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.
A selective inhibitor of SIRT1 over SIRT2 and SIRT3

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Indoles and derivatives
Subclass Carbazoles
Intermediate Tree Nodes Not available
Direct Parent Carbazoles
Alternative Parents 3-alkylindoles  Benzenoids  Aryl chlorides  Pyrroles  Heteroaromatic compounds  Primary carboxylic acid amides  Azacyclic compounds  Organopnictogen compounds  Organonitrogen compounds  Organochlorides  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Carbazole - 3-alkylindole - Indole - Aryl chloride - Aryl halide - Benzenoid - Heteroaromatic compound - Pyrrole - Carboxamide group - Primary carboxylic acid amide - Carboxylic acid derivative - Azacycle - Organonitrogen compound - Organochloride - Organohalogen compound - Hydrocarbon derivative - Organic oxide - Carbonyl group - Organopnictogen compound - Organic oxygen compound - Organooxygen compound - Organic nitrogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.
External Descriptors Not available

Associated Targets(Human)

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

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HD1 Histone deacetylase (38 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Ube2d3 Ubiquitin-conjugating enzyme E2 D3 (38 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504763229
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504763229
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)
InChIKey FUZYTVDVLBBXDL-UHFFFAOYSA-N
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
Molecular Weight 248.71
Reaxy-Rn 416178
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=416178&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

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

7 results found

Lot Number Certificate Type Date Item
K2230732 Certificate of Analysis Sep 12, 2024 E129892
K2230738 Certificate of Analysis Sep 12, 2024 E129892
K2230708 Certificate of Analysis Sep 12, 2024 E129892
K2230599 Certificate of Analysis Sep 12, 2024 E129892
K2230667 Certificate of Analysis Sep 12, 2024 E129892
K2230583 Certificate of Analysis Sep 12, 2024 E129892
A1527018 Certificate of Analysis Jun 13, 2024 E129892

Chemical and Physical Properties

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).
Sensitivity Heat Sensitive
Refractive Index 1.69
Boil Point(°C) 531.72°C/760mmHg
Melt Point(°C) 178°C
Molecular Weight 248.710 g/mol
XLogP3 2.500
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 1
Rotatable Bond Count 1
Exact Mass 248.072 Da
Monoisotopic Mass 248.072 Da
Topological Polar Surface Area 58.900 Ų
Heavy Atom Count 17
Formal Charge 0
Complexity 323.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 1
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Citations of This Product

How to Cite Aladdin Scientific Products?
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   
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). 
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). 
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). 
5. Xinlin Chen, Lihong Hong, Ying Wu, Yucheng Gu, Jianguang Luo, Lingyi Kong.  (2024)  A dual recognition-based strategy employing Ni-modified metal-organic framework for in situ screening of SIRT1 inhibitors from Chinese herbs.  TALANTA,  274  (125975). 

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