| Identification | Back Directory | [Name]
LY411575 | [CAS]
209984-57-6 | [Synonyms]
CS-509
LY411575
LY4114575
LSN-411575
LY411575, >=98%
LY411575;LY 411575
LY-411575 >=97% (HPLC)
LY-411575;LY411575; LY 411575
LY411575, 98%, a γ-secretase inhibitor
(S)-2-((S)-2-(3,5-Difluorophenyl)-2-hydroxyacetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dib
(S)-2-(2-(3,5-difluorophenyl)acetaMido)-N-((S)-5-Methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanaMide
(S)-2-((S)-2-(3,5-Difluorophenyl)-2-hydroxyacetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propanamide
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
(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
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 | [Molecular Formula]
C26H23F2N3O4 | [MDL Number]
MFCD09832551 | [MOL File]
209984-57-6.mol | [Molecular Weight]
479.48 |
| Chemical Properties | Back Directory | [Boiling point ]
836.0±65.0 °C(Predicted) | [density ]
1.40 | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble5mg/mL, clear | [form ]
powder | [pka]
11.79±0.20(Predicted) | [color ]
white to beige | [InChIKey]
ULSSJYNJIZWPSB-CVRXJBIPSA-N |
| Hazard Information | Back Directory | [Description]
γ-Secretase is a multi-subunit aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules. One well-known substrate of this enzyme is Notch, a transmembrane receptor that plays a key role in cell fate decisions including cell proliferation, differentiation, and apoptosis. LY411575 is a cell-permeable γ-secretase inhibitor (IC50 = 0.14 nM) that has been shown to block Notch activation in vitro at 500 μM.1,2 LY411575 can induce apoptosis in Kaposi’s sarcoma cells as well as promote intestinal goblet cell differentiation in a mouse model of colitis.2,3 It has also been observed to promote neural differentiation of mouse embryonic stem cells.4 | [Uses]
LY-411575 has been used as a potent γ-secretase inhibitor and Notch inhibitor. | [Definition]
ChEBI: A dibenzoazepine that is 5,7-dihydro-6H-dibenzo[b,d]azepin-6-one which is substituted at the 7 pro-S position by the C-terminal carboxamide nitrogen of N
/element>2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]-L-alaninamide. It is a potent, cell permeable and selective gamma-secretase inhibitor. It has been tested as a possible treatment
for Alzheimer's disease and shows promise for its potential to counteract severe hearing loss. | [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. | [target]
γ-secretase | [storage]
Store at -20°C | [References]
[1] EVA CZIRR. Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.[J]. The Journal of Biological Chemistry, 2007, 282 34: 24504-24513. DOI: 10.1074/jbc.m700618200
[2] CHRISTINE L CURRY. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in Kaposi”s sarcoma tumor cells[J]. Oncogene, 2005, 24 42: 6333-6344. DOI: 10.1038/sj.onc.1208783
[3] RYUICHI OKAMOTO. Requirement of Notch activation during regeneration of the intestinal epithelia.[J]. American journal of physiology. Gastrointestinal and liver physiology, 2009, 296 1: G23-35. DOI: 10.1152/ajpgi.90225.2008
[4] ELSA ABRANCHES. Neural differentiation of embryonic stem cells in vitro: a road map to neurogenesis in the embryo.[J]. PLoS ONE, 2009: e6286. DOI: 10.1371/journal.pone.0006286 |
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