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

CAS: 208255-80-5 Cat. No.: D408190 Peso molecular: 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

Descripción general

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

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Nombres e identificadores

• Isómeros 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 Alemania: 3
• CAS alternativo: 208255-80-5
• Términos de entrada MeSH: 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
• Peso molecular: 432.46
• Reaxy-Rn: 24866565
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24866565&ln=

Propiedades químicas y físicas

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

Referencias

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7. Peipei Li, Jing Kang, Xiaojie Wu, Duo Wang, Yongjun Li, Nan Liang, Rui Du, Minjie Wang, Alideertu Dong, Yuliang Li.  (2024)  Mild phototherapy strategies for efficient treatment of bacterial keratitis while avoiding side effects.  Nano Today,      [PMID:] [10.1016/j.nantod.2024.102336]

8. Li Na, Mao Jingwei, Tang Haiying, Tan Xiaoyan, Bi Jian, Wu Hao, Chen Xiuli, Wang Yingde.  (2025)  FLT3 ligand regulates expansion of regulatory T-cells induced by regulatory dendritic cells isolated from gut-associated lymphoid tissues through the Notch pathway.  CHINESE MEDICAL JOURNAL,      [PMID:40211734] [10.1097/CM9.0000000000003493]