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Merck

E7034

Sigma-Aldrich

EX-527

≥98% (HPLC), SIRT1 and SIRT6 inhibitor, powder

동의어(들):

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

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C13H13ClN2O
CAS 번호:
49843-98-3
Molecular Weight:
248.71
MDL number:
MFCD03009471
UNSPSC 코드:
12352200
PubChem Substance ID:
329799003
NACRES:
NA.77

주요 문서

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제품 이름

EX-527, ≥98% (HPLC)

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: >20 mg/mL

저장 온도

2-8°C

SMILES string

NC(=O)C1CCCc2c1[nH]c3ccc(Cl)cc23

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

관련 카테고리

애플리케이션

EX-527 has been used:
  • in 1% dimethyl sulfoxide, 30%, polyethylene glycol-400 and 1% Tween 80 for treating C57BL/6 N mice to study its effect on intestinal morphological changes and crypt cell apoptosis
  • as a an inhibitor of sirtuin 1, in treating human cancer lines MCF-7 (Michigan cancer foundation-7) and HCT116 (colon cancer cell line) incubated in Dulbecco′s modified Eagle′s medium, to study its effect on mitochondrial ATP (adenosine triphosphate) production
  • Intracerebroventricularly infused in rat model of epileptogenesis, to access kainic acid–induced status epilepticus stimulated sirtuin 1 activity

생화학적/생리학적 작용

EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.
Potent SIRT1 and SIRT6 inhibitor.

특징 및 장점

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number
027M4719V
105M4730V
084M4710V
113M4725V
013M4733V

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특정 버전이 필요한 경우 로트 번호나 배치 번호로 특정 인증서를 찾을 수 있습니다.

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문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

Hong-Xia Liu et al.
Experimental cell research, 357(2), 271-281 (2017-05-30)
Mitochondrial trifunctional protein α-subunit (MTPα) is involved in the fatty acid β-oxidation (FAO) pathway. Two MTPα activities, 3-hydroxyacyl-CoA dehydrogenase and long-chain hydratase, have been linked with the occurrence and development of obesity and obesity-related disorders. These activities catalyze two steps
A Rise in ATP, ROS, and Mitochondrial Content upon Glucose Withdrawal Correlates with a Dysregulated Mitochondria Turnover Mediated by the Activation of the Protein Deacetylase SIRT1
Song S and Hwang E
Cells, 8(1), 11-11 (2019)
Takahito Abe et al.
The Journal of reproduction and development, 63(5), 455-461 (2017-06-13)
Resveratrol is a potent activator of NAD-dependent deacetyltransferase sirtuin-1 (SIRT1) and affects lipid metabolism and ATP generation in somatic cells. In the present study, the effects of supplementing culture medium with resveratrol on lipid metabolism, ATP generation, and cryosensitivity of
The Role of Sirt1 in Epileptogenesis
Hall Alicia M, et al.
eNeuro, 4(1) (2017)
The protective effects of Resveratrol against radiation-induced intestinal injury
Zhang H, et al.
BMC Complementary and Alternative Medicine, 17(1), 410-410 (2017)
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We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

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