DAPT (GSI-IX)
DAPT (GSI-IX)
| 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：2159513211 |
| DAPT (GSI-IX) |
CFN60023 |
208255-80-5 |
5mg |
QQ客服：2159513211 |
| DAPT (GSI-IX) |
CFN60023 |
208255-80-5 |
10mg |
QQ客服：2159513211 |
| DAPT (GSI-IX) |
CFN60023 |
208255-80-5 |
20mg |
QQ客服：2159513211 |
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Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.
IF=36.216(2019)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.
IF=14.548(2019)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
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国外学术期刊发表的引用ChemFaces产品的部分文献
| 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. |
|
|
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 |
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
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