DAPT (GSI-IX) - Moligand™, 10mM in DMSO , CAS No.208255-80-5

CAS: 208255-80-5 Cat. No.: D408190 分子式: C₂₃H₂₆F₂N₂O₄ 分子量: 432.46

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

LY-374973 | (S)-tert-butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

DAPT (GSI-IX, LY-374973) is a novelγ-secretaseinhibitor, which inhibits Aβ production withIC50of 20 nM in HEK 293 cells. DAPT enhances theapoptosisof human tongue carcinoma cells and regulatesautophagy.
In vitro

In human primary neuronal cultures, DAPT also shows inhibitory effects on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ total and Aβ42, which is 5-10-fold lower than is observed in HEK 293 cells. A recent study shows that DAPT inhibits the proliferation of SK-MES-1 cells in a concentration-dependent manner with IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and caspase-independent apoptosis in lung squamous cell carcinoma cells by inhibiting Notch receptor signaling pathway.

In vivo

DAPT administration (100mg/kg) leads to a robust and sustained pharmacodynamic effect in PDAPP mice that DAPT levels in the brain exceeds 100 ng/g within 1 hour and persists up to 18 hours after administration, with peak levels of 490 ng/g observed after 3 hour. And during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ and Aβ42 in a dose-dependent manner with a 50% reduction. In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced activity of γ-secretase and increases the cell apoptosis with the prolonged neuroinflammation.
Cell Data

cell lines：

Concentrations：2.5 μM to 160 μM

Incubation Time：72 hours

Powder Purity:≥98%

Specifications

同義語

LY-374973 | (S)-tert-butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

DAPT (GSI-IX, LY-374973) 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.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

名前と識別子

• 異性体SMILES: C[C@@H](C(=O)N[C@@H](C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
• WGKドイツ: 3
• 代替CAS番号: 208255-80-5
• MeSH用語: DAPT butylester;DAPT peptide;GSI-IX cpd;N-(2FPhAc)Ala-phenyl-Gly t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)-S-phenylglycine t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)phenylglycine t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)phenylgly
• 分子量: 432.46
• Reaxy-Rn: 24866565
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24866565&ln=

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 27 mg/mL (199.82 mM)

参考文献

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