Grouped product items

SKU

Size

Availability

Price

Qty

E129892-5mg

5mg

In stock

$53.90

E129892-10mg

10mg

Available within 4-8 weeks(?)

$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

Basic Description

Synonyms	49843-98-3 \| Selisistat \| 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide \| EX-527 \| EX 527 \| SEN0014196 \| SIRT1 Inhibitor III \| Selisistat [INN] \| EX527 \| EX 527 (Selisistat) \| Selisistat (EX 527) \| CHEMBL420311 \| CHEBI:90369 \| rac-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-
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. A selective inhibitor of SIRT1 over SIRT2 and SIRT3

Associated Targets(Human)

SIRT2 Tchem NAD-dependent protein deacetylase sirtuin-2 (3 Activities)

Discover Target: SIRT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SIRT1 Tchem NAD-dependent protein deacetylase sirtuin-1 (26 Activities)

Discover Target: SIRT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)

Discover Target: ABL1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)

Discover Target: GSK3B

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CSNK1D Tchem Casein kinase I delta (4546 Activities)

Discover Target: CSNK1D

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)

Discover Target: CYP2D6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)

Discover Target: CDK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)

Discover Target: CYP1A2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)

Discover Target: CYP2C9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)

Discover Target: CYP2C19

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)

Discover Target: CYP3A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

YES1 Tclin Tyrosine-protein kinase YES (2781 Activities)

Discover Target: YES1

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)

Discover Target: AURKA

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)

Discover Target: SIRT3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SIRT2 Tchem NAD-dependent deacetylase sirtuin 2 (3979 Activities)

Discover Target: SIRT2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SIRT1 Tchem NAD-dependent deacetylase sirtuin 1 (3505 Activities)

Discover Target: SIRT1

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)

Discover Target: CD38

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)

Discover Target: BRD4

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)

Discover Target: SIRT5

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)

Discover Target: TRIM24

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

BRPF1 Tchem Peregrin (2217 Activities)

Discover Target: BRPF1

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)

Discover Target: UBE2T

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)

Discover Target: Mapk1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)

Discover Target: Fgfr3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HD1 Histone deacetylase (38 Activities)

Discover Target: HD1

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)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Ube2d3 Ubiquitin-conjugating enzyme E2 D3 (38 Activities)

Discover Target: Ube2d3

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

Sarm1 NAD(+) hydrolase SARM1 (23 Activities)

Discover Target: Sarm1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

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

Database links

PubChem CID	5113032
CAS Registry No.	49843-98-3
ChEMBL Ligand	CHEMBL420311

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

7 results found

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

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

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

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]

References

1. Blander G, Guarente L. (2004) The Sir2 family of protein deacetylases.. Annu Rev Biochem, 73 (3): (417-35). [PMID:15189148]
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]
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]
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. 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]
7. 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]
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]

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

Basic Description

Associated Targets(Human)

Associated Targets(non-human)

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

Safety and Hazards(GHS)

Related Documents

Citations of This Product

References

Solution Calculators

Molarity Calculator

Dilution Calculator

Reconstitution Calculator