DAPT (GSI-IX)

	产品编号	CFN60023
	CAS编号	208255-80-5
	分子式 = 分子量	C₂₃H₂₆F₂N₂O₄ = 432.46
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源
ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用

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产品名称	产品编号	CAS编号	包装	QQ客服
DAPT (GSI-IX)	CFN60023	208255-80-5	1mg	QQ客服：3257982914
DAPT (GSI-IX)	CFN60023	208255-80-5	5mg	QQ客服：3257982914
DAPT (GSI-IX)	CFN60023	208255-80-5	10mg	QQ客服：3257982914
DAPT (GSI-IX)	CFN60023	208255-80-5	20mg	QQ客服：3257982914

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ChemFaces的产品在许多优秀和顶级科学期刊中被引用

Cell. 2018 Jan 11;172(1-2):249-261.e12.
doi: 10.1016/j.cell.2017.12.019.
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PMID: 29328914

Cell Metab. 2020 Mar 3;31(3):534-548.e5.
doi: 10.1016/j.cmet.2020.01.002.
IF=22.415(2019)

PMID: 32004475

Mol Cell. 2017 Nov 16;68(4):673-685.e6.
doi: 10.1016/j.molcel.2017.10.022.
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PMID: 29149595

ACS Nano. 2018 Apr 24;12(4): 3385-3396.
doi: 10.1021/acsnano.7b08969.
IF=13.903(2019)

PMID: 29553709

Nature Plants. 2016 Dec 22;3: 16206.
doi: 10.1038/nplants.2016.205.
IF=13.297(2019)

PMID: 28005066

Sci Adv. 2018 Oct 24;4(10): eaat6994.
doi: 10.1126/sciadv.aat6994.
IF=12.804(2019)

PMID: 30417089

Sapienza University of Rome (Italy)

University of Melbourne (Australia)

University of Madras (India)

National Cancer Institute (USA)

University of Cincinnati (USA)

Imperial College London (United Kingdom)

Kazusa DNA Research Institute (Japan)

University of the Basque Country (Spain)

VIT University (India)

University of Lodz (Poland)

Leibniz Institute of Plant Biochemistry (Germany)

Instituto de Investigaciones Agropecuarias (Chile)

Helmholtz Zentrum München (Germany)

Institute of Bioorganic Chemistry Polish Academy of Sciences (Poland)

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Description:

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.

Targets:

γ-secretase | Aβ | Autophagy

In vivo:

Neuroscience,2012 May 17;210:99-109.

The γ-secretase blocker DAPT impairs recovery from lipopolysaccharide-induced inflammation in rat brain.[Pubmed: 22445932]

γ-Secretase is an important contributing enzyme in Alzheimer's disease and is therefore an important therapeutic target. However, the impact of γ-secretase inhibition is not well studied in acute neuroinflammation induced by systemic infection.
METHODS AND RESULTS:
In this study the influence of γ-secretase on the expression of some proinflammatory markers was assessed in the acute phase as well as the subsiding phase of neuroinflammation. Cerebral γ-secretase cleavage activity was measured by a fluorometric assay after lipopolysaccharide (LPS) intraperitoneal administration. Time profiles of TNF-α and COX-II expression were then determined to detect the time points relevant to the maximal inflammatory responses and the subsequent recovery phase. γ-Secretase activity coincident with TNF-α protein expression returned to its basal level till 8-12 h after systemic challenge with low dose LPS while COX-II over expression lasted for 48-72 h later. Pharmacological inhibition of γ-secretase with local or systemic administration of DAPT (N-[N-(3,5-difluorophenacetyl)-l-alanyl]-S-phenylglycine t-butyl ester) was performed to indicate the results on the developmental and sinking phases of inflammatory responses in 6 and 72 h post LPS respectively. Our results demonstrate that both local and systemic modulation of γ-secretase hyper-activity with DAPT increase the duration of TNF-α, COX-II, and NFκB induction. We consistently found mild augmented apoptosis in animals treated with DAPT as determined by measuring cleaved caspase-3 expression and by TUNEL assay 72 h following LPS injection.
CONCLUSIONS:
These results suggest that γ-secretase modulation interferes with certain immune regulatory pathways which may restrict some inflammatory transcription factors such as NF-κB.

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	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.3124 mL	11.5618 mL	23.1235 mL	46.2471 mL	57.8088 mL
5 mM	0.4625 mL	2.3124 mL	4.6247 mL	9.2494 mL	11.5618 mL
10 mM	0.2312 mL	1.1562 mL	2.3124 mL	4.6247 mL	5.7809 mL
50 mM	0.0462 mL	0.2312 mL	0.4625 mL	0.9249 mL	1.1562 mL
100 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.4625 mL	0.5781 mL