209984-57-6

Basic information

• Product Name: LY411575
• Synonyms: LY411575;(aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide;(S)-2-(2-(3,5-difluorophenyl)acetaMido)-N-((S)-5-Methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanaMide;Benzeneacetamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-α-hydroxy-, (αS)-;(aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide LY 411575;LY 411575 (aS)-N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-alpha-hydroxybenzeneacetamide;LSN-411575;N2-[(2S)-2-(3,5-Difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide
• CAS NO: 209984-57-6
• Molecular Formula: C26H23F2N3O4
• Molecular Weight: 479.481
• Product Categories: Inhibitor;Inhibitors
• Mol File: 209984-57-6.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 836.0±65.0 °C(Predicted)
• Appearance: white to beige/
• Density: 1.40
• Storage Temp.: ?20°C
• Solubility: DMSO: soluble5mg/mL, clear
• PKA: 11.79±0.20(Predicted)
• CAS DataBase Reference: LY411575(CAS DataBase Reference)
• NIST Chemistry Reference: LY411575(209984-57-6)
• EPA Substance Registry System: LY411575(209984-57-6)

Safety Data

• Safety Statements: 24/25
• WGK Germany: 3
• Hazardous Substances Data: 209984-57-6(Hazardous Substances Data)

Usage

Description

LY411575 is a dibenzoazepine compound that acts as a potent and selective γ-secretase inhibitor and Notch inhibitor. It is a cell-permeable molecule with an IC50 of 0.14 nM, which has demonstrated the ability to block Notch activation in vitro at 500 μM. LY411575 has shown potential in various applications, including the treatment of Alzheimer's disease and counteracting severe hearing loss.

Uses

Used in Pharmaceutical Applications:
LY411575 is used as a γ-secretase inhibitor for the potential treatment of Alzheimer's disease. It targets the γ-secretase enzyme, which is involved in the proteolytic cleavage of substrates, including the amyloid precursor protein (APP). Inhibition of this enzyme can help reduce the formation of amyloid-beta peptides, which are associated with the development of Alzheimer's disease.
Used in Hearing Loss Treatment:
LY411575 is used as a potential treatment for severe hearing loss. It has been observed to promote neural differentiation of mouse embryonic stem cells, which could potentially be applied to restore or improve hearing function in individuals with hearing loss.
Used in Cancer Research:
LY411575 is used as a Notch inhibitor for cancer research. Notch signaling plays a crucial role in cell fate decisions, including cell proliferation, differentiation, and apoptosis. By inhibiting Notch activation, LY411575 can induce apoptosis in Kaposi’s sarcoma cells, providing a potential therapeutic approach for cancer treatment.
Used in Intestinal Health Research:
In a mouse model of colitis, LY411575 is used as a promoter of intestinal goblet cell differentiation. This application suggests that the compound may have potential in the treatment or management of inflammatory bowel diseases by promoting the regeneration and maintenance of the intestinal epithelium.

Biochem/physiol Actions

LY-411575 is potent, cell permeable and selective γ-secretase inhibitor that reduces Aβ/42 after acute or chronic treatment, and blocks Notch activation. Studies (Cancer Cell) have shown that treatment with LSN-411575 arrests KrasG12V-driven NSCLCs in association with inhibition of HES1 expression and ERK phosphorylation.